RSP 601

RSP Amino Acids, LLC 2007-2008 Building Block Index Structural Index, Version 6.
01
RSP Amino Acids, LLC 87 Squannacook Road Shirley, MA 01464 USA email: rsp@amino-acids.com web address: http://www.amino-acids.com T:978-448-3911, F:978-448-2914
RSPs Structural Index, Version 6.01 for 2007-2008
The Company
RSP Amino Acids, LLC, is committed to providing fast, reliable service and superior-quality analogues for the discovery of new medicines, biomaterials, and research tools. RSP Amino Acids, LLC, is a custom amino acid product company. We use asymmetric process research and development to make market select amino acid analogues. For over nine years, RSP has led worldwide, commercial expansion of new chiral amino acids through continuous investments in chemical product research, development, and marketing. We focus on carefully selected analogues, diverse properties, and useful functional groups for basic and advanced studies in medicine, biochemistry, and molecular biology. RSPs business is enabled by our market selection pipeline for sharing knowledge and consolidating molecular opinions, for the indexing of new amino acids. We encourage you to continue to help RSP, yourself, and your customers by looking at our pipeline and voting on the most useful amino acids across fifteen different core fields under market selection at www.amino-acids.com. All scientists are welcome to submit their ideal research amino acids for consideration. RSPs Business Beliefs x The majority of new drugs with improved toxicological and efficacy profiles will use and contain new and unusual amino acids. x Diversity coverage of advanced chiral space can be hampered by long, difficult, and expensive syntheses. Broad and in-depth process knowledge allows RSP to solve our customers most difficult problems. x The bedrock of our beliefs is that process development chemistry will always rescue and win the challenge of creating satisfactory economies of scale for manufacturing.
TO PLACE AN ORDER: Telephone: 978-448-3911 Internet: Mail: Fax: 978-448-2914
http://www.amino-acids.com E-mail: rsp@amino-acids.com RSP Amino Acids LLC Accounts, Mark Cava 87 Squannacook Road Shirley, MA 01464 U.S.A.
When ordering please have the following information: Billing and shipping addresses; quotation number; catalogue number; name including stereochemistry; quantity of material ordered; any special analytical requirements; and purchase order number (P.O. #) OFFICE HOURS: Monday - Friday: 8 A.M. - 6 P.M. EDT Weekends & US Holidays: Closed Orders may be placed at any time by phone, fax, or email.
Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com
Contents
A Letter to Our Customers Capabilities Graphic Illustration Customer & Technical Service How To Find a Product Purity Pricing Bulk Quantities and Design Services Terms Payments
Rights and License
4 5 6 6 6 6 6 7 7
7
Warranties Cancellations Index by RSP Number
7 7 8
Amino Acid Building Blocks and Scaffolds

Aliphatic amino acids (alkane, alkene, alkyne, and cyclic) Single Ring Aromatic Amino Acids (e.g., substituted Phg, Phe, and Tyr) Polycyclic Aromatic Amino Acids Single ring heterocyclic amino acids Polycyclic heteronuclear amino acids Amino and Alkylamino Containing Side Chains (e.g., Lys) Carboxyl, carboxamide, and carboxyl ester group containing side chains Guanidine and Amidine Containing Side Chains (e.g., Arg) Hydroxy and alkoxy containing side chains Non-D amino acids (E-amino acids, etc.) Amino acids lacking either the D-amino or carboxyl groups (amino alcohols and D-hydroxy acids) 10 13 26 27 36 38 44 46 48 49 50
Dear Colleague, RSP Amino Acids, LLC, is pleased to introduce our Building Block Index, Version 6.01 for 2007-2008. Version 6.01 includes 677 molecules, an increase of 30 new amino acid projects since Version 5.01. The indexs structural information is also available in .db, .sdf, and excel formats. To bring you this information, RSP invests all profits in R&D and operates with more than half of its output focused on new, research, amino acids. Therefore, if you like the work we are doing and would like to see it continue, please contact us today about becoming a customer. RSPs 6.01 index contains the most highly selected property from our pipeline of building blocks and intermediates. Our market selection results have been cross-pollinated with worldwide medicinal chemical opinion for over nine years. The respondents range from prizewinners to young scientists. The contents of version 6.01 are the best selections from this stochastic process. The results of this survey are evident in the many new and emerging applications using RSP amino acids to sculpt key advancements in science and medicine. There are three ways to do business with RSP: 1. Open Market Building Block Index Version 6.01: You can submit a quote-request for any property, and we will fax it with price and availability (stock or offer). If it is in stock and beyond price supports, then you can buy it from 100 mg up. You can solicit quotes by phone, fax or internet. It is convenient to login at www.amino-acids.com, go to products to search part numbers, access structures, and request quotes through the RFQ dialogue. 2. Syndicated Buyers of Products and Derivatives: RSPs amino acid analogues are active in current projects across the majority of therapeutic areas for small molecule, protein and peptidomimetic drug leads. Funded synthesis projects are quoted from milligrams to kilograms. All quotes on new syntheses carry variable price support at the customers minimum. We are open to bulk amino acid and associated fragment business including tech- transfer for manufacturing. 3. Closed-Market Capabilities (see graphic illustration on next page): RSPs indexed alpha amino acids and pipeline candidates make up our open-market product platform. RSPs closed-market, custom, business leverages our significant skill at amino acid chemistry. This approach provides access to a spectrum of futures analogues including carboxamides, diamines, diacids, beta B2 or B1 amino acids, amino alcohols, amino aldehydes, -amino aldehydes, des-NH2(H or Me), des-COOH(H or Me), 12-, 11-, 2- and methyl substituted amino acids, bicyclic scaffolds, N-alkylated amino acids, and pseudopeptido-mimetic variants (e.g, aa-(R-NH2)-aa1). Custom intermediates through finished products can be contracted as straight fee-for-service or with process transfer rights. We also provide extra value through exclusivities for applied process developmentjust ask. At RSP, we strictly separate our open- and closed-market analogue businesses; this lets us maintain nondisclosure. For our customers, we promise to provide honest and regular communications, confidentiality, innovative solutions, and high quality. Before we call on you, please take a few minutes now to write down a couple of important questions you have about myself, our company, its chemists, or our record and forward them to email(rsp@aminoacids.com), through Special Requests at www.amino-acids.com, by fax, or just call us at 978-448-3911. We wish you continued success in business and research! Sincerely,
Mark Cava
President
RSP Amino Acids, LLC
RSPs closed-market capabilities help our customers tailor amino acid functionality for medicinal chemistry
Boc Boc N N
Boc N
Prg N H O
Prg N H O
Prg N H
NH2
Boc N
N Boc
Prg N H
O
Boc N
N
R
O Boc
OH
Boc N
Prg N H
OH
Prg N H O
OH Prg N H
O Prg N H
Prg N H
OH
N Boc Boc N
N R2 R1 Prg N H OH R3 O Boc
N Boc Boc N
O Prg N H OH
Prg N Me O
OH
CUSTOMER & TECHNICAL SERVICE Phone:978-448-3911, Fax: 978-448-2914, email: rsp@amino-acids.com, and web: www.amino-acids.com HOW TO FIND A PRODUCT RSPs amino acid analogues are indexed by RSP amino acid property classes Index number (see Index by RSP Number for structural classifications, contents and endpaper) Structure (see Index by RSP Number for structural property classes). PURITY The analytical purity of amino acid analogues sold by RSP is 97+% unless otherwise stated. We normally quote lot history or current QC as a guide on quotes, usually 97+%, 98+% and 99+% depending on process maturity. Purity is determined by HPLC. Optical purity is determined by a variety of methods. Detailed information about characterization of each compound is given on the analytical data sheet supplied with each compound. If your application requires quality assurance of ee%>=99 or 99.5% of a single isomer, then ask us to quote special service specifications and analytical requirements. We consistently achieve high ees through process development and enantiomeric enrichment techniques. PRICING RSPs book-pricing is based on availability and demand. Available compounds are a large discount from project costs. New synthesis prices are dependent on demand and process maturity. You can solicit quotes directly by phone, fax or internet. Login at www.amino-acids.com and go to products to search part numbers, access structures, and request quotations from the RFQ dialogue. We fax quotes with price and availability (stock or offer). If the compound is in stock and beyond price support, then you can buy it from 100 mg up at gram list price. If the analogue is subject to customersupported minimum order quantities, we will offer you the minimum. Price support protects our customers new molecular property acquisitions. Price support also ensures access to the same property, by all, at the customer-supported minimum. BULK QUANTITIES AND DESIGN SERVICES RSP bulk services offers amino acid analogues x From hundreds of grams to five kilogram quantities x With different protection schemes x With high or enhanced chemical and enantiomeric purities x In single lots or by standing order (with scaled cancellation terms) Please call (978-448-3911) for quotes on your special needs.
TERMS Terms are net 20 days. Overdue accounts are subject to a 1.5% monthly service charge (18% annual charge). Quotes are valid for 30 days. After 30 days or as indicated, please call for a re-quote. All prices are subject to change, but no product will be shipped at an increased price without notification. RSP reserves the right to charge a 35% restocking fee on returned goods due to an ordering mistake. This is used to cover assay costs. In all cases call customer service (978-448-3911) for a return authorization number. Items returned without an authorization number will not be accepted. Unless otherwise agreed, quoted orders for indexed custom products or custom syntheses are noncancellable, nonguarranteed deliverables (see below). All synthesis quotes carry cancellation options. At the customers request orders received before 11 AM eastern standard time, will be shipped F.O.B. by FedEx, Airborne Express, or UPS. Check with RSPs customer service for shipment by other carriers. All products are sold for experimental use only and are not for drug or clinical use. RSP Amino Acids, LLC, cannot be held responsible to damages arising from the misuse of any product. PAYMENTS Please call 978-448-3911 for any questions. Send payments to: Mail or overnight express: RSP Amino Acids, c/o Mark Cava, Accounts, 87 Squannacook Road, Shirley, MA 01464. Wire payments: Call for instructions and please refer to the Sales Order Number on the invoice when making wire payments. Delivery Versus Payment (DVP) discounts require a pro-forma invoice. Credit card: Please call Mark Cava at 978-448-3911 for payment by AMEX, VISA or MC credit cards. Prices are in $US dollars. Prices do not include taxes, duties, and insurance charges. Quoted prices are FOB destination in the form of a packing and handling charge. RIGHTS AND LICENSE RSP reserves all rights on any product prepared or procedure developed in our laboratories. WARRANTIES RSP warrants its products to be of the stated quality at the time of sale. It is the buyers responsibility to determine the adequacy of all materials for any intended use or purpose. It is RSPs obligation to replace material up to the amount of the purchase price. This applies to products in the original container and may not apply to a product that has been tampered with or altered in any way or has been misused or damaged by accident or through negligence. If a customer is not satisfied with the quality of our products, we will replace them.
CANCELLATIONS
Unless otherwise agreed, all orders for indexed custom products or custom syntheses are noncancellable, nonguarranteed deliverables subject to re-stocking and cost of goods allowance.
INDEX BY RSP NUMBER Numbers used for RSPs amino acid analogues refer to the structure of the final amino acid after all protecting groups are removed. They fall into the categories listed below. Within each category, amino acid analogues are numbered in order of acquisition. 0000-0999 1000-2999 3000-3499 3500-4499 4500-4999 5000-5499 5500-5999 6000-6499 6500-6999 7000-7499 7500-7999 8000-8499 8500-8999 9000-9999 aliphatic amino acids (alkane, alkene, alkyne, and cyclic) single ring aromatic amino acids polycyclic aromatic amino acids single ring heterocyclic amino acids polycyclic heteronuclear amino acids amino and alkyl amino group containing side chains carboxyl, carboxamide, and carboxyl ester group containing side chains guanidine and amidine group containing side chains hydroxy and alkoxy containing side chains mercapto and alkylmercapto containing side chains other heteroatom containing side chains D-imino acids non-D amino acids (E-amino acids, etc.) amino acids lacking either the D-amino or carboxyl groups (amino alcohols and Dhydroxy acids)
Protecting groups are shown as suffixes to the number used to indicate the structure of each analogue. Each protecting group is assigned a one letter code in the order D-amino, side chain, D-carboxyl protecting groups. An 3-character suffix is used when there is a possibility of confusion. Subscript numbers following the letter indicate the number of protecting groups. Fmoc-Tyr(tBu): Fmoc-Tyr-tBu: Tyr(tBu)-OFm Fmoc-Phe [4-Guanido(Boc)2] RSP-1706-fu RSP-1706-fou RSP-1706-ouf RSP-6006-fb2
RSP number abbreviations for analogue protection

Group Boc Tosyl Ethyl Methyl Pmc 2-Br-Benzyloxy 1,3-dioxane* Letter b s e m p r ac Group Fmoc trityl Benzyloxy t-butyl Benzoyl S-trityl Benzyl Letter f t z u bz st bn
* dioxane nomenclature is used for aldehyde protection (e.g., the full acetal of Fmoc-L-Phe(4-CHO) or 1666-fac)
Building Blocks and Scaffolds

RSP Amino Acids, LLC Version 6.01 Index
Chiral Chiral Z N H O OH NH2 O ClH O OH Boc N H O Boc N H O O
Chiral
Z-D-2-Aminobutyric Acid 0014-Z
D,L-3-Amino-ethylpentinoate-HCL 0025
Boc-(2R)-2-amino-5-hexenoic acid 0034-b
Boc-(2R)-2-amino-5-hexenoic acid, methylester 0034-bm
Chiral
Chiral
Chiral
Chiral
H2 N O
OH
Boc
N H O
OH
Boc
N H O
Fmoc
N H O
OH
(2S)-2-amino-5-hexenoic acid 0036
(2S)-Boc-2-amino-5-hexenoic acid 0036-b
(2S)-Boc-2-amino-5-hexenoic acid methylester 0036-bm
(2S)-Fmoc-2-amino-5-hexenoic acid 0036-f
Chiral
Chiral
Chiral
Chiral
H2 N O
OH
Boc
N H O
OH
OH Fmoc N H O H2 N O OH
(2S)-2-amino-6-heptenoic acid 0046
(2S)-Boc-2-amino-6-heptenoic acid 0046-b
(2S)-Fmoc-2-amino-6-heptenoic acid 0046-f
(2S)-2-amino-7-octenoic acid 0056
Chiral
Chiral
Chiral
Chiral
Boc
N H
OH O
Fmoc
N H
OH O
Boc
N H
OH O
Fmoc
N H
OH O
(2S)-Boc-2-amino-7-octenoic acid 0056-b
(2S)-Fmoc-2-amino-7-octenoic acid 0056-f
(2S)-Boc-2-amino-8-nonenoic acid 0066-b
(2S)-Fmoc-2-amino-8-nonenoic acid 0066-f
10
Chiral Chiral HO O N Boc H H2 N O O Boc Chiral OH O O O Chiral
N H
H2 N
Boc-(2S)-2 amino-9-decenoic acid 0076-b
(2R)-Gly(2-cyclopropyl)-OMe 0084-om
Boc-(2S)-Gly(2-cyclopropyl) 0086-b
(2S)-Gly(2-cyclopropyl)-OMe 0086-om
NH3 O
OH
HN Boc
COOH
HN
COOH Fmoc
NH3 ClH O
1,1-accp 0093
Boc-1, 1-accp 0093-b
Fmoc-1, 1-accp 0093-f
1, 1-accp(OMe) 0093-om
Chiral
Chiral
Chiral
Chiral
Boc
N H
OH O
H2 N O
Boc
N H
OH O
H2 N O
Boc-(2R)-Gly(2-cyclobutyl) 0094-b
(2R)-Gly(2-cyclobutyl)-OMe 0094-om
Boc-(2S)-Gly(2-cyclobutyl) 0096-b
(2S)-Gly(2-cyclobutyl)-OMe 0096-om
OH O HN
OH O Boc
OH O Fmoc H2 N
O O
H2 N
HN
1,1-accb 0103
Boc-1, 1-accb 0103-b
Fmoc-1,1-accb 0103-f
1, 1-accb(OMe) 0103-om
11
Boc N O O O
H N
O P O O N
O O O
Z H N
tBu O O
Bp-Gly-OtBu Schiff Base 0116-Bpu
Boc-(2R, 2S)-Gly[PO(OMe)2]-OMe 0126-Bmm
Bp-(2R, 2S)-Gly(2-OAc)-OMe 0136-Bpam
Z-Gly-OtBu 0146-zu
Chiral OH H2 N O N Boc N H O Chiral O O HN Z O O O HN Boc OH O
(1S, 2S)-pseudoephedrine glycinamide 0156
Boc-(2R, 2S)-Gly(2-OMe)-OMe 0165-bmm
Z-(2R, 2S)-Gly(2-OMe)-OMe 0165-zmm
Boc-D-Ala(3-cyclopropyl) 0174-b
Chiral OH HN Fmoc O H2N
Chiral O O H2 N
Chiral OH HN O Boc
Chiral OH O
Fmoc-D-Ala(3-cyclopropyl) 0174-f
D-Ala(3-cyclopropyl)OMe 0174-om
L-Ala(3-cyclopropyl) 0176
Boc-L-Ala(3-cyclopropyl) 0176-b
Chiral OH HN Fmoc O H2N
Chiral O HN O Boc
Chiral OH O HN
Chiral OH O Fmoc
Fmoc-L-Ala(3-cyclopropyl) 0176-f
L-Ala(3-cyclopropyl)OMe 0176-om
Boc-D-Ala(3-cyclobutyl) 0184-b
Fmoc-D-Ala(3-cyclobutyl) 0184-f
12
Chiral O H2 N HN O Boc
Chiral OH O HN
Chiral OH O Fmoc H2 N
Chiral O O
D-Ala(3-cyclobutyl)OMe 0184-om
Boc-L-Ala(3-cyclobutyl) 0186-b
Fmoc-L-Ala(3-cyclobutyl) 0186-f
L-Ala(3-cyclobutyl)OMe 0186-om
Chiral O H H NH2 COOH H H Boc N H O OH
H2 N O
HN Z O
(2R, 2S)-Gly[2-cyclohexyl(4-oxo, full Et-ketal)-OMe 0196-oacm
Z-(2R, 2S)-Gly[2-cyclohexyl(4-oxo, full Et-ketal)-OMe 0196-zacm
2,2-aminocarboxy-adamantane 0206
Boc-(2S)-2-amino-heptanoic acid 0216-b
Chiral
Chiral
Chiral
Chiral
H2 N O
OH
HN Boc O
OH H2N O
OH HN Boc O
OH
D-Ala-3-Cyclopentane 0224
Boc-D-Ala-3-Cyclopentyl 0224-b
L-Ala-3-cyclopentyl 0226
Boc-L-Ala(3-cyclopentyl) 0226-b
Chiral
Chiral
tBu
OH
Chiral
Boc
N H O
OH
Fmoc
N H O
OH Fmoc N H O OH H2N O
OH
Boc-L-Phg 1006-b
Fmoc-L-Phg 1006-f
Fmoc-D, L-norTyr(tBu) 1015-fu
L-norTyr 1016
13
OH
Chiral
OH
Chiral
tBu Chiral
Fmoc N H
Boc
N H O
OH
Fmoc
N H O
OH
Fmoc
N H O
OH
Boc
N H O
OH
Boc-L-norTyr 1016-b
Fmoc-L-norTyr 1016-f
Fmoc-L-norTyr(tBu) 1016-fu
Boc-D, L-Phg(4-CH2NH-Fmoc) 1045-bf
Boc N H Fmoc
H N
Chiral Boc
H N
Chiral
Boc HN
Chiral
Fmoc
N H O
OH
Boc
N H O
OH
Fmoc
N H O
OH
H2 N O
OH
Fmoc-D, L-Phg(4-CH2NHBoc) 1045-fb
Boc-L-Phg(4-CH2NH-Fmoc) 1046-bf
Fmoc-L-Phg(4-CH2NHBoc) 1046-fb
L-Phg(4-CH2NH-Boc) 1046-ob
H Fmoc N
Chiral
O S
O O NaH
Boc
Chiral
Boc
Chiral NH
H2N O
OH
Fmoc
N H O
OH
Fmoc
N H O
OH
Fmoc
N H O
OH
L-Phg(4-CH2NH-Fmoc) 1046-of
Fmoc-D,L-Phg(4-CH2-SO3Na) 1055-f
Fmoc-L-Phg(4-NH-Boc) 1066-fb
Fmoc-L-Phg(3-CH2NHBoc) 1076-fb
Chiral H O Fmoc OH N H O OH OH N Boc Chiral O NH2 O H O OH H N Boc O tBu
Boc-L-Phe 1506-b
Fmoc-L-Phe 1506-f
D, L-m-Tyr 1515
Boc-D, L-m-Tyr(tBu) 1515-bu
14
Chiral H O OH N Fmoc OH O tBu H2N O OH HN Boc O
OH Chiral H O OH OH N Boc O tBu Chiral
Fmoc-D, L-m-Tyr(tBu) 1515-fu
L-m-Tyr 1516
Boc-L-m-Tyr 1516-b
Boc-L-m-Tyr(tBu) 1516-bu
H O
Fmoc
Chiral OH O
Fmoc O
Chiral O
NH2 O OH
Chiral O
Boc
Chiral O
OH
OH
tBu
OH
Fmoc-L-m-Tyr 1516-f
Fmoc-L-m-Tyr(tBu) 1516-fu
L-m-Tyr(Me) 1526
Boc-L-m-Tyr(Me) 1526-b
H O
Fmoc
Chiral O O
H NH2 O OH OH
Boc O
Fmoc
OH
OH
mom
OH
OH
Fmoc-L-m-Tyr(Me) 1526-f
D, L-o-Tyr 1535
Boc-D, L-o-Tyr(mom) 1535-bmom
Fmoc-D, L-o-Tyr 1535-f
H O
Fmoc
HO
Chiral H O N Boc Chiral O OH
Boc
Chiral
OH
mom
H2 N O
OH OH
OH
O mom
Fmoc-D, L-o-Tyr(mom) 1535-fmom
L-o-Tyr 1536
Boc-L-o-Tyr 1536-b
Boc-L-o-Tyr(mom) 1536-bmom
15
Chiral O O mom
Chiral H O H2N OH O OH O N Boc Chiral O OH O H N Fmoc Chiral
Fmoc
H N O OH
Fmoc-L-o-Tyr(mom) 1536-fmom
L-o-Tyr(Me) 1546
Boc-L-o-Tyr(Me) 1546-b
Fmoc-L-o-Tyr(Me) 1546-f
H O
Boc
I Chiral O
Fmoc
I Chiral O
HN
Fmoc
H Chiral NH2 O N O
Chiral
OH
OH
OH
OH
Boc-L-Phe(4-I) 1556-b
Fmoc-L-Phe(4-I) 1556-f
Fmoc-L-Phe(4-Me) 1566-f
L-Phe(4-NHAc) 1576
H H O OH N Boc N O
Chiral H O OH N Fmoc
H N O
Chiral HN O OH Fmoc
tBu S O OH H N Fmoc
tBuChiral S
Boc-L-Phe(4-NH-Ac) 1576-b
Fmoc-L-Phe(4-NHAc) 1576-f
Fmoc-D, L-Phe(4-S-tBu) 1585-fu
Fmoc-L-Phe(4-S-tBu) 1586-fu
tBuChiral NH2 O OH S O OH H N Fmoc
H N Boc O OH HN Boc
BocChiral NH O OH H N Boc
H N
Chiral Fmoc
L-Phe(4-S-tBu) 1586-ou
Fmoc-D, L-Phe(4-NH-Boc) 1595-fb
Boc-L-Phe(4-NH-Boc) 1596-bb
Boc-L-Phe(4-NH-Fmoc) 1596-bf
16
H H O OH N Fmoc N Boc
Chiral NH2 O OH
BocChiral NH O OH NH2
H N
Chiral Fmoc O O
NH2
NH2 Chiral
Fmoc-L-Phe(4-NH-Boc) 1596-fb
L-Phe(4-NH-Boc) 1596-ob
L-Phe(4-NH-Fmoc) 1596-of
L-Phe(4-NH2)-obn 1596-oobn
ClChiral
ClChiral H O N Boc ClChiral O OH O OH H N Fmoc CN
H2 N O
OH
H2 N
OH
D-Phe(4-Cl) 1604
L-Phe(4-Cl) 1606
Boc-L-Phe(4-Cl) 1606-b
Fmoc-D, L-Phe(4-CN) 1615-f
Fmoc NH2 O OH CNChiral O OH H N Boc CNChiral O O OH OH H N Fmoc CNChiral H N Boc
L-Phe(4-CN) 1616
Boc-L-Phe(4-CN) 1616-b
Fmoc-L-Phe(4-CN) 1616-f
Boc-D, L-Phe(4-CH2NH-Fmoc) 1625-bf
N Alloc H Fmoc N H O OH O OH H N Fmoc
Boc
H HN O OH Boc
HN
BocChiral H O OH N Boc
Fmoc
HChiral
Fmoc-D, L-Phe(4-CH2NH-Alloc) 1625-fa
Fmoc-D, L-Phe(4-CH2NH-Boc) 1625-fb
Boc-L-Phe(4-CH2NH-Boc) 1626-bb
Boc-L-Phe(4-CH2NH-Fmoc) 1626-bf
17
Alloc H O OH N Fmoc
HChiral H O OH N Fmoc
Boc
HChiral
Chiral N Alloc H H2 N O OH O OH NH2
Boc
HChiral
Fmoc-L-Phe(4-CH2NH-Alloc) 1626-fa
Fmoc-L-Phe(4-CH2NH-Boc) 1626-fb
L-Phe(4-CH2NH-Alloc) 1626-oa
L-Phe(4-CH2NH-Boc) 1626-ob
HN NH2 O OH
FmocChiral H O OH N Fmoc
O O
Chiral O
Boc
NO2Chiral O
Fmoc
NO2Chiral
tBu
OH
OH
L-Phe(4-CH2NH-Fmoc) 1626-of
Fmoc-L-Phe(4-COO-tBu) 1636-fu
Boc-L-Phe(4-NO2) 1646-b
Fmoc-L-Phe(4-NO2) 1646-f
tBuChiral H O OH N Fmoc O O OH H N Boc
BrZChiral O O OH H N Fmoc
tBuChiral O O OH H N Fmoc
O H
Fmoc-D-Tyr(tBu) 1654-fu
Boc-L-Tyr(BrZ) 1656-br
Fmoc-L-Tyr(tBu) 1656-fu
Fmoc-D, L-Phe(4-CHO) 1665-f
O O O Fmoc N H O OH H N Boc
O H
O Chiral O
Chiral O H O N Fmoc H Chiral
Boc OH
N H O
OH
OH
Fmoc-D, L-Phe[4-(1,3-dioxane)] 1665-fac
Boc-L-Phe(4-CHO) 1666-b
Boc-L-Phe[4-(1,3-dioxane)] 1666-bac
Fmoc-L-Phe(4-CHO) 1666-f
18
O O
Chiral
O O
Chiral Chiral H OH O O OH N Boc Chiral
Fmoc
N H O
OH
H2 N O
OH
H2N
Fmoc-L-Phe[4-(1,3-dioxane)] 1666-fac
L-Phe[4-(1,3-dioxane)] 1666-oac
L-Phe(4-Et) 1676
Boc-L-Phe(4-Et) 1676-b
Chiral H O OH N Fmoc O OH NH2
Chiral H O OH N Boc
Chiral H O OH N Fmoc
Chiral
Fmoc-L-Phe(4-Et) 1676-f
L-Phe(4-iPr) 1686
Boc-L-Phe(4-iPr) 1686-b
Fmoc-L-Phe(4-iPr) 1686-f
Chiral
Chiral Fmoc H
Chiral Boc N N H O OH N S Fmoc
TrtChiral
Boc
N H O
OH
Fmoc
N H O
OH
O OH
Boc-L-Tyr(Me) 1696-b
Fmoc-L-Tyr(Me) 1696-f
Fmoc-L-Phe(4-CH2NiPr-Boc) 1706-fb
Fmoc-L-Phe(4-CH2-S-Trt) 1716-ft
S NH2 O OH
TrtChiral H O OH N Boc
O NH2 O OH H N Fmoc
O NH2 O OH NH2
Chiral NH2
L-Phe(4-CH2-S-Trt) 1716-t
Boc-D, L-Phe(4-C(O)NH2) 1725-b
Fmoc-D, L-Phe(4-C(O)NH2) 1725-f
L-Phe(4-C(O)NH2) 1726
19
O NH O OH
Chiral H NH2 O OH N Boc
Chiral NH2 O OH H N Fmoc
Chiral NH2 O OH NH2
CN
N-Ac-L-Phe(4-C(O)NH2) 1726-ac
Boc-L-Phe(4-C(O)NH2) 1726-b
Fmoc-L-Phe(4-C(O)NH2) 1726-f
D,L-Phe(4-CH2-CN) 1735
CN H O OH N Boc O OH HN Fmoc
CN H O OH N Boc
H N O O S O OH HN Fmoc
H N O O S
Boc-D,L-Phe(4-CH2-CN) 1735-b
Fmoc-D,L-Phe(4-CH2-CN) 1735-f
Boc-D, L-Phe(4-NH-SO2-CH3) 1745-b
Fmoc-D, L-Phe(4-NH-SO2-CH3) 1745-f
H NH2 O OH N O O S
Chiral H O OH N Boc
H N O O S
Chiral HN O OH Fmoc
H N O O S
Chiral NH2 O OH
Chiral O
L-Phe(4-NH-SO2-CH3) 1746
Boc-L-Phe(4-NH-SO2-CH3) 1746-b
FmocL-Phe(4-NH-SO2-CH3) 1746-f
L-Phe(4-COCH3) 1756
Chiral H O OH N Boc O O H N Fmoc
Chiral O H2 N OH O OH
BrChiral
BrChiral
H2 N O
OH
Boc-L-Phe(4-COCH3) 1756-b
Fmoc-L-Phe(4-COCH3) 1756-f
D-Phe(4-Br) 1764
L-Phe(4-Br) 1766
20
Br O O O OH OH OH HO F F F O Chiral H N Boc O NO2 H N Fmoc O NO2 NH2 NO2 Chiral
H2N
L-Phe(4-Br)-O-bn, TFA salt 1766-obn
Boc-D, L-Phe(3-NO2) 1775-b
Fmoc-D, L-Phe(3-NO2) 1775-f
L-Phe(3-NO2) 1776
NO2 Chiral H O OH N Boc O OH H N Fmoc
NO2 Chiral O
Boc
F Chiral O
Boc
F Chiral
OH
OH
Boc-D-Phe(4-F) 1784-b
Boc-L-Phe(4-F) 1786-b
H O
Fmoc
F Chiral HN Fmoc
H N
Boc
Chiral NH2 O OH NO2
Chiral O
HN
Boc
Chiral
OH
O OH
OH
NO2
Fmoc-L-Phe(4-F) 1786-f
Fmoc-L-Phe(3-CH2NH-Boc) 1796-fb
L-Phe(2-NO2) 1806
HN O
Fmoc
Chiral
OH
Trt
OH
Fmoc OH NO2
N H O
OH
Fmoc
N H O
OH
H2 N O
tBu
Fmoc-D, L-Phe(4-CH2-OH) 1845-f
Fmoc-D, L-Phe(4-CH2-O-Trt) 1845-ft
D, L-Phe(4-CH2-OH)-OtBu 1845-ouo
21
OH
Chiral
Chiral OH
BocChiral
TrtChiral
H2 N O
OH
Fmoc
N H O
OH
Fmoc
N H O
OH
Fmoc
N H O
OH
L-Phe(4-CH2-OH) 1846
Fmoc-L-Phe(4-CH2-OH) 1846-f
Fmoc-L-Phe(4-CH2-O-Boc) 1846-fb
Fmoc-L-Phe(4-CH2-O-Trt) 1846-ft
TrtChiral H Boc
OH Chiral O S O N H O OH OH N Fmoc
OH Chiral O S O H O OH N Boc
OH O S O
H2N O
OH
L-Phe(4-CH2-O-Trt) 1846-ot
Boc-D-Phe(4-CH2-SO3H) 1854-b
Fmoc-D-Phe(4-CH2-SO3H) 1854-f
Boc-D, L-Phe(4-CH2-SO3H) 1855-b
OH O S O H O OH N Fmoc O OH H N Boc
OH Chiral O S O H O OH N Fmoc
OH Chiral O S O Boc O OH N H SO3 HChiral
Fmoc-D, L-Phe(4-CH2-SO3H) 1855-f
Boc-L-Phe(4-CH2-SO3H) 1856-b
Fmoc-L-Phe(4-CH2-SO3H) 1856-f
Boc-D-Phe(4-SO3H) 1864-b
bn O H O OH N Fmoc S Chiral OH O O OH O H N Boc S Chiral OH O O O OH O O H N Fmoc S Chiral OH O H N Boc
Chiral bn
O P O
Fmoc-D-Phe(4-SO3H) 1864-f
Boc-L-Phe(4-SO3H) 1866-b
Fmoc-L-Phe(4-SO3H) 1866-f
Boc-D-Phe[4-CH2-PO3(bn)2]-OMe 1874-bbn2m
22
bn
Chiral bn H O OH N Fmoc
O P O H O N Boc
NO2 F
Chiral Boc NH O OH
Chiral NO2 O
F H N Fmoc
Chiral NO2
OH
Boc-L-Phe[4-CH2-PO3(bn)2]-OMe 1876-bbn2m
Fmoc-L-Phe(4-F, 3-NO2) 1886-f
Boc-L-Phe(3-F, 4-NO2) 1896-b
Fmoc-L-Phe(3-F, 4-NO2) 1896-f
OH HN O OH Fmoc
Chiral
O OH
O O N N N NH NH2 N N NH N Boc
Chiral OH
OH
N N N NH
Fmoc
NH
NH
Fmoc-L-Phe(3, 5-dihydroxy) 1906-f
Fmoc-D, L-Phe[4-(5-tetrazoyl)] 1925-f
D, L-Phe[4-(5-tetrazoyl)]-OMe 1925-om
Boc-L-Phe[4-(5-tetrazoyl)] 1926-b
OH O Chiral OH N N N NH Fmoc NH O
Fmoc NH O
O NH2 O
OH
BocChiral NH
NH
NH
N N
N N
NH N N
Fmoc-L-Phe[4-(5-tetrazoyl)] 1926-f
Fmoc-D, L-Phe[4-(5-tetrazoyl)] 1935-f
D, L-Phe[3-(5-tetrazoyl)] 1935-om
Boc-L-Phe[4-(5-tetrazoyl)] 1936-b
OH O
FmocChiral NH O N N OH Fmoc NH O N N NH Boc N Chiral OH O N N N OH FmocChiral NH
N N
NH
N N
N N
Fmoc-L-Phe[4-(5-tetrazoyl)] 1936-f
Fmoc-D, L-Ala-3-(2-N-tetrazoyl) 1945-f
Boc-L-Ala-3-(2-N-tetrazoyl) 1946-b
Fmoc-L-Ala-3-(2-N-tetrazoyl) 1946-f
23
OH O N N N NH
FmocChiral NH H N N O
OH
Fmoc NH H N N O
OH
BocChiral NH H N N
OH O
FmocChiral NH
Fmoc-L-Ala-3-(5-N-tetrazoyl) 1956-f
Fmoc-D, L-Ala-3-(5-benzimidazoly) 1965-f
Boc-L-Ala-3-(5-benzimidazoly) 1966-b
Fmoc-L-Ala-3-(5-benzimidazoly) 1966-f
Boc O
NH
Chiral ClChiral H N HN O O O H O OH Boc O Chiral NH O O HN Tfa ClChiral
OH HN HN
O O NH
HN
Tfa
Boc-L-Phe[4-amino(N-L-hydroorotyl) 1976-b
Tfa-L-Phe(4-CH2-Cl)-OMe 1976-tm
Boc-D-Phe[4-amino(N-t-butylcarbamoyl) 1984-b
Tfa-L-Phe(3-CH2-Cl)-OMe 1986-t
NH2 H O OH N Fmoc OH Chiral Cl O OH H Fmoc BnChiral O Cl O H OH N H O OH NO2 H N Boc Chiral OH OH
Chiral
Fmoc-L-Tyr(3-Cl) 2006-f
Fmoc-L-Tyr(Bn, 3-Cl) 2006-fbn
Boc-L-Tyr(3-NO2) 2026-b
L-Tyr(3-NH3) 2036
OH H O OH N Boc B OH O OH H N Fmoc
OH B OH O OH NH2
OH B OH
Chiral H O OH N Boc
OH Chiral B OH
Boc-D, L-Phe[4-B(OH)2] 2045-b
Fmoc-D, L-Phe[B(OH)2] 2045-f
L-Phe[B(OH)2] 2046
Boc-L-Phe[4-B(OH)2] 2046-b
24
OH H O NH OH Boc Fmoc N H COOH H2 N Fmoc OH Chiral B OH HO COOH
OH Chiral
COOH
Fmoc-L-Phe[B(OH)2] 2046-f
Boc-D, L-Tyr(2,6-di-Me) 2055-b
Fmoc-D, L-(2,6-di-Me)Tyr 2055-f
L-Tyr(2,6-di-Me) 2056
Chiral OH Chiral OH Chiral O Si OH Chiral
COOH Boc N H HN
COOCH3 Boc HN
COOH COOH Boc Fmoc N H
Boc-L-Tyr(2,6-di-Me) 2056-b
Boc-L-Tyr(2,6-di-Me)-OMe 2056-bom
Boc-L-Tyr(2,6-diMe, TBDS)-OH 2056-bTBDPSo
Fmoc-L-(2,6-di-Me)Tyr 2056-f
Chiral H O OH N Boc I O OH H N Fmoc I I H2 N O OH OH O H N Boc I Chiral
Boc-D, L-Phe(3-I) 2065-b
Fmoc-D, L-Phe(3-I) 2065-f
L-Phe(3-I) 2066
I H O OH N Fmoc I Chiral Boc N H COOH O I OH I H2 N O OH H N Fmoc
Chiral
Boc-D, L-Phe(2-I) 2075-b
Fmoc-D, L-Phe(2-I) 2075-f
L-Phe(2-I) 2076
25
H O
Boc
Chiral O
Fmoc
Chiral H O N Boc
HN
Fmoc H O N
HN Fmoc
Alloc
OH
OH
I OH OH
Boc-D, L-Phe(3-NH-Fmoc) 2085-bf
Fmoc-D, L-Phe(3-NH-Alloc) 2085-fa
HN HN O OH Fmoc
Boc
HN
Alloc
Boc Chiral NH H O N Boc
HN
FmocChiral
H2 N O
OH Boc N H O
OH
OH
Fmoc-D, L-Phe(3-NH-Boc) 2085-fb
D, L-Phe(3-NH-Alloc) 2085-oa
Boc-L-Phe(3-NH-Boc) 2086-bb
Boc-L-Phe(3-NH-Fmoc) 2086-bf
HN H O OH N Fmoc
BocChiral NH2 O OH
HN
BocChiral NH2 O OH
HN
FmocChiral
O O S O O O NH2
Chiral NH2
Fmoc-L-Phe(3-NH-Boc) 2086-fb
L-Phe(3-NH-Boc) 2086-ob
L-Phe(3-NH-Fmoc) 2086-of
L-Phe(3-NH2)-O-bn, 2 p-Tosylate salt 2086-oobn
HO
O NH
Chiral H2 N COOH F Chiral
Fmoc HN COOH F
Chiral
NH Chiral 2
Fmoc F F OH F OH F OH Boc N H OH O
Fmoc-L-Tyr(3,5-diFluoro) 2096-f
L-Tyr(2,6-diFluoro) 2106
Fmoc-L-Tyr(2,6-diFluoro) 2106-f
Boc-L-Phe(3-C(O)NH2) 2126-b
26
Chiral
Chiral
Chiral O
Chiral
Boc
N H O
OH
Boc
N H O
OH
Fmoc
N H O
OH
Fmoc
N H
OH O
Boc-D-hPhe 2504-b
Boc-L-hPhe 2506-b
Fmoc-L-hPhe 2506-f
Fmoc-L-hTyr(mom) 2516-fmom
Trt
Chiral
Chiral
Chiral
NO2
Fmoc
N H
OH O
Boc
N H
OH O
Fmoc
N H
OH O
Fmoc
N H
OH O
Fmoc-L-hTyr(Trt) 2516-ft
Boc-L-hTyr(Me) 2526-b
Fmoc-L-hTyr(Me) 2526-f
Fmoc-D, L-hPhe(4-NO2) 2535-f
NO2Chiral
NO2
Chiral Chiral NO2 O H N Boc O OH OH H N Fmoc Chiral
Fmoc
N H
OH O
Fmoc
N H
OH O
Fmoc-L-hPhe(4-NO2) 2536-f
Fmoc-L-hPhe(2, 4-di-NO2) 2546-f
Boc-L-Phe(4-Ph) 3026-b
Fmoc-L-Phe(4-Ph) 3026-f
H O
Boc
Chiral HO O Z
tBu O
Chiral OH O
Chiral OH O
Chiral OH O
OH
N H
N H
N Fmoc
N Boc
[(Z-L-Phe)(Boc-L-Phe)]ether 3036-bz
L-transPro(4-OtBu) 3506-ouo
Fmoc-D-Pro(4-oxo) 3514-f
Boc-L-Pro(4-oxo) 3516-b
27
Chiral O O O
O O O
Chiral
Chiral OH O
CN
Chiral N H OH O
N Boc
N Boc
N Fmoc
Boc-L-Pro(4-oxo)-O-bn 3516-bobn
Boc-L-Pro(4-oxo)-OMe 3516-bom
Fmoc-L-Pro(4-oxo) 3516-f
L-transPro(4-CN) 3526
CN
Chiral OH O
CN O O
Chiral Bn
CN
Chiral O O
CN
Chiral OH O
N Boc
N Boc
N Boc
N Fmoc
Boc-L-transPro(4-CN) 3526-b
Boc-L-transPro(4-CN)-OBn 3526-bobn
Boc-L-transPro(4-CN)-OMe 3526-bom
Fmoc-L-transPro(4-CN) 3526-f
O H
Chiral
HO OH O
Chiral
HO
Chiral OH O
HO
Chiral OH O
N Fmoc O
OH
N H
N Boc
N Fmoc
Fmoc-L-transPro(4-CHO) 3536-f
L-transPro(4-CH2OH) 3546
Boc-L-transPro(4-CH2OH) 3546-b
Fmoc-L-transPro(4-CH2OH) 3546-f
Boc NH
Chiral
Fmoc NH
Chiral
Alloc N H N Fmoc O
Chiral
Boc N H
Chiral
N Boc O
OH N Boc O
OH
OH
N Fmoc O
OH
Boc-L-transPro(4-CH2NH-Boc) 3556-bb
Boc-L-transPro(4-CH2NH-Fmoc) 3556-bf
Fmoc-L-transPro(4-CH2NH-Alloc) 3556-fa
Fmoc-L-transPro(4-CH2NH-Boc) 3556-fb
28
Chiral
H2N O
OH
Boc
N H O
OH Fmoc N H O
OH
Boc
N H O
OH
D, L-homo(Ala-4-Pyr) 75%S & 25%R (scalemic) 3565(50ee)
Boc-D, L-homo(Ala-4-Pyr) 3565-b
Fmoc-D, L-homo(Ala-4-Pyr) 3565-f
Boc-L-homo(Ala-4-Pyr) 3566-b
Chiral Alloc H N Chiral OH O Boc H N Chiral OH O F F Chiral OH O
Fmoc
N H O
OH
N Fmoc
N Fmoc
N Boc
Fmoc-L-homo(Ala-4-Pyr) 3566-f
Fmoc-L-transPro(4-NH-Alloc) 3566-fa
Fmoc-L-transPro(4-NH-Boc) 3566-fb
Boc-D-Pro(4,4-difluoro) 3574-b
Chiral OH O
Chiral OH O
Chiral O O
CN
Chiral OH O
N Fmoc
N Boc
N Boc
N Fmoc
Fmoc-D-Pro(4,4-difluoro) 3574-f
Boc-L-Pro(4,4-difluoro) 3576-b
Boc-L-Pro(4,4-difluoro)-OMe 3576-bom
Fmoc-L-transPro(4-CH2CN) 3576CN-f
HO F F Chiral OH O N H Chiral CO2 H N H Chiral CO2H N Fmoc O
Chiral
N Fmoc
OH
Fmoc-L-Pro(4,4-difluoro) 3576-f
L-Azetidine-2-Carboxylic acid 3586
L-homoPro 3596
Fmoc-L-transPro[4-(4-Phenol)] 3596-f
29
Chiral ClH N H Chiral S H2N O OH H2 N O S OH N Fmoc O OH
Chiral
COOCH3
L-homoPro-OMe-HCl 3596-m
D, L-Ala-[3-(2-Thienyl)] 3605
L-Ala-[3-(2-Thienyl)] 3606
Fmoc-L-transPro(3-Ph) 3616-f
O bn H N
Chiral Trityl S Chiral OH O N Fmoc O
Chiral O
tBu
Chiral
N Fmoc O
OH
N Fmoc
OH
N Fmoc O
OH
Fmoc-L-transPro(4-(NH-(CH2-CO-bn) 3626-fbn
Fmoc-L-Pro(4-S-trityl) 3636-ft
Fmoc-L-transPro(4-Ph) 3646-f
Fmoc-L-transPro[4-COOtBu)] 3656-fu
N N N N H N Fmoc O
Chiral O N H Chiral O OH O N Chiral O O N Chiral O
OH
Boc OH
Fmoc OH
Fmoc-L-transPro(4-tetrazoyl) 3666-f
(3S)-morpholine carboxylic acid 3676
N-Boc-Morpoline[(3S)-COOH)] 3676-b
N-Fmoc-Morpoline[(3S)-COOH)] 3676-f
H N N
Z ClH Chiral O N N
Chiral
Boc N
Chiral
Boc N ClH Chiral O OMe
Boc OMe
Boc OH
Fmoc OH
N H
[(2-N-Boc)Piperizine(2R)COOH]-OMe, HCl 3684-bom
N-Boc-[(4-N-Z)Piperazine(2R)COOH] 3684-bz
N-Fmoc-[(4-N-Boc)Piperazine(2R)COOH ] 3684-f
[(4-N-Boc)Piperizine(2R) COOH]-OMe, HCl 3684-obm
30
Boc N O N H
Chiral
Alloc N N O
Boc N N Boc
Chiral
H N N
ClH Chiral O
COOH
OH
Fmoc OH
Boc OMe
[(4-N-Boc)Piperizine(2R) COOH 3684-obo
N-Fmoc-[(4-N-Alloc)Piperazine(2S,2R)C OOH] 3685-fa
N-Boc-[(4-N-Boc)Piperazine(2S)COOH 3686-bb
[(2-N-Boc)Piperazine(2S)COOH]-OMe, HCl 3686-bom
Z N N
Chiral
Boc N
Chiral
Boc N ClH
Chiral
OMe N
Chiral
Boc
Boc OH
Fmoc OH
N H
O OMe S O
N-Boc-[(4-N-Z)Piperazine(2S)COOH 3686-bz
Fmoc-(2S)-Piperazinyl(4-N-Boc) 3686-fb
[(4-N-Boc)Piperizine(2S) COOH]-OMe, HCl 3686-obm
Boc-L-transPro(4-p-tolylthiocarbonyl)-O Me 3696-bsm
O O
Chiral
I Ts O Chiral Bn S N OH O H2N O Boc N H O S
N Trityl O
N Boc
N OH
Trityl-L-transPro(4-COOMe)-OMe 3696-tmm
Boc-L-transPro(OTs)-Obn 3706-btsbn
D, L-Ala-3-[2-(5-iodo)thiazole)] 4005
Boc-D, L-Ala-3-[2-(5-iodo)thiazole)] 4005-b
I S N Fmoc N H OH H2N O O S
N I S OH H2N Boc O N H O
N I S OH
N O
Fmoc-D, L-Ala-3-[2-(5-iodo)thiazole)] 4005-f
D, L-Ala-3-[2-(5-iodo)thiazole)]-OMe 4005-om
31
N I S Fmoc N H OH O O OH NH2 N
I I N S Boc N H OH O Fmoc N H S N
I S
OH O
H2N N
O H N Chiral
H N N
Chiral H N Chiral N N OH Fmoc O N N OH N H O Chiral
Fmoc N H O
OH
Fmoc N H O
Boc OH
N H
Fmoc-L-Ala-4-[5-(2-amino)imidazoyl] 4036-f
Fmoc-L-Ala-4-[5-(2-acetamido)imidazoyl] 4036-face
Boc-L-Ala-3-(2-pyrimidinyl) 4046-b
Fmoc-L-Ala-3-(2-pyrimidinyl) 4046-f
Chiral N OH
Chiral N OH H O HO O N Fmoc Chiral
Alloc
H N
Chiral
Boc
N H
Fmoc O
N H
N Boc O
Boc-L-Ala-3-(5-pyrimidinyl) 4056-b
Fmoc-L-Ala-3-(5-pyrimidinyl) 4056-f
Fmoc-L-Ala-3-(3-furanyl) 4066-f
Boc-L-transPro(CH2CH2-NH-Alloc)-OM e 4076-bam
O Boc H N Chiral
OH Chiral NH
OH NH N
Chiral
Chiral O O NH2 N
N FmocO
OH
Boc
Fmoc
OH
OH
OH
Fmoc-L-transPro(4-CH2CH2NH-Boc) 4076-fb
Boc-L-Ala-[3-(6-(3-hydroxypyridine))] 4086-b
Fmoc-L-Ala-[3-(6-(3-hydroxypyridine))] 4086-f
L-Ala-[3-(6-(3-hydroxypyridine))]OMe 4086-om
32
O N O
Chiral
O N O
Chiral
OH Chiral NH
OH NH N
Chiral
OH HN Boc HN
OH Fmoc N
Boc N
Fmoc
Boc-L-Ala-[3-(4-N-Morpholine)] 4096-b
Fmoc-L-Ala-[3-(4-N-Morpholine)] 4096-f
Boc-L-Ala-[3-(4-pyrimidinyl)] 4106-b
Fmoc-L-Ala-[3-(4-pyrimidinyl)] 4106-f
Boc HO
NH
Chiral
Fmoc HO
NH
Chiral
Chiral HO
Fmoc NH
NH N
O NH N
Boc
N H
OH O O
Boc-L-Ala-[3-(3-pyrazoyl)] 4116-b
Fmoc-L-Ala-[3-(3-pyrazoyl)] 4116-f
Boc-(2R)-Gly-4-Pyranoyl 4124-b
Fmoc-(2S, 2R)-Gly-4-Pyranoyl 4125-f
O O NH2 HO
BocChiral NH
O HO
FmocChiral NH HO O
OH
BocChiral NH
(2S, 2R)-Gly-4-Pyranoyl-OMe 4125-om
Boc-(2S)-Gly-4-Pyranoyl 4126-b
Fmoc-(2S)-Gly-4-Pyranoyl 4126-f
Boc-L-Ala-[3-(5-(3-hydroxypyridinoyl))] 4136-b
OH O HO N
FmocChiral NH O HO N
O NH2
Chiral H2N N Fmoc S O H2N OH NH N Boc S NH O Chiral OH
Fmoc-L-Ala-[3-(5-(3-hydroxypyridinoyl))] 4136-f
L-Ala-[3-(5-(3-hydroxypyridinoyl))]-OMe 4136-om
Fmoc-D, L-Ala-3-[5-(2-amino)thiazoyl] 4145-f
Boc-L-Ala-3-[5-(2-amino)thiazoyl] 4146-b
33
H2N N
S NH
O Chiral OH H2 N N S
OH N Fmoc H H2 N N S
OH
Chiral H2N N S
OH
Chiral
Fmoc
N Boc H
N Fmoc H
Fmoc-L-Ala-3-[5-(2-amino)thiazoyl] 4146-f
Fmoc-(2S, 2R)-Gly-2-[5-(2-amino)thiazoyl] 4155-f
Boc-(2S)-Gly-2-[5-(2-amino)thiazoyl] 4156-b
Fmoc-(2S)-Gly-2-[5-(2-N-amino)thiazoyl] 4156-f
OH O O H N Fmoc N Alloc N Boc
OH H N Fmoc N Boc O
O NH2
OH O H N Boc N Fmoc
Chiral
Fmoc-(2S, 2R)-Gly-2-[3-(N-Alloc-pyrroyl)] 4165-fa
Fmoc-(2S, 2R)-Gly-2-[3-(N-Boc-pyrroyl)] 4165-fb
(2S, 2R)-Gly-2-[3-(N-Boc-pyrroyl)]-OMe 4165-om
Boc-(2S)-Gly-2-[3-(N-Fmoc-pyrroyl)] 4166-bf
OH O H N
Chiral O
OH H N
Chiral
Fmoc NH
Chiral
H N AllocChiral
Fmoc N Alloc N Boc
Fmoc N Boc O OH O N Fmoc OH
Fmoc-(2S)-Gly-2-[3-(N-Alloc-pyrroyl)] 4166-fa
Fmoc-(2S)-Gly-2-[3-(N-Boc-pyrroyl)] 4166-fb
Boc-L-(4-cis/trans)-homoPro(4-CH2NH-F moc) 4176-bf
Fmoc-L-(4-cis/trans)-homoPro(4-CH2NHAlloc) 4176-fa
Boc NH
Chiral
H N
NH2 N O OH NH H2 N N Boc O H N NH Chiral OH H2 N N Fmoc H N NH O Chiral OH
O Fmoc
Fmoc OH
Fmoc-L-(4-cis/trans)-homoPro(4-CH2NHBoc) 4176-fb
Fmoc-D, L-His(2-NH2) 4185-f
Boc-L-His(2-NH2) 4186-b
Fmoc-L-His(2-NH2) 4186-f
34
OH
OH
OH
OH
HN Boc
COOH
HN
COOH
HN Boc
COOH
HN
COOH
Fmoc
Fmoc
Boc-(4-cis/trans)-1, 1-acch(4-COOH) 4193-b
Fmoc(4-cis/trans)-1, 1-acch(4-COOH) 4193-f
Boc-(4-cis/trans)-1, 1-acch(4-CH2OH) 4203-b
Fmoc(4-cis/trans)-1, 1-acch(4-CH2OH) 4203-f
OH
OH
Chiral
Chiral
HN Boc
COOH
HN
COOH
N Boc
O OH
Fmoc
Fmoc OH
Boc(4-cis/trans)-1, 1-acch(4-OH) 4213-b
Fmoc(4-cis/trans)-1, 1-acch(4-OH) 4213-f
Boc-L-homoPro(4-oxo) 4226-b
Fmoc-L-homoPro(4-oxo) 4226-f
F F
Chiral
F F
Chiral
Chiral
HN
Fmoc
Chiral
N Boc
O OH
N H
O O N Boc COOH
Fmoc OH
Boc-L-homoPro(4,4-difluoro) 4236-b
Fmoc-L-homoPro(4,4-difluoro) 4236-f
L-homoPro(4,4-difluoro)-OMe 4236-om
Boc-L-transhomoPro(4-NH-Fmoc) 4246-bf
HN
Alloc
Chiral
HN
Boc
Chiral
HN
Boc ClH
Chiral
OH
Chiral
N Fmoc
COOH
N Fmoc
COOH
N H
O N O boc
O OH
Fmoc-L-transhomoPro(4-NH-Alloc) 4246-fa
Fmoc-L-transhomoPro(4-NHBoc) 4246-fb
L-transhomoPro(4-NHBoc)-OMe 4246-obm
Boc-L-(4-cis/trans)-homoPro(4-CH2OH) 4256-b
35
OH
O Chiral OH O N Boc
Chiral
O OH
Chiral Chiral O O N
Fmoc OH
COOH
N Fmoc
COOH
Fmoc-(2S)-(4-cis/trans)-homoPro(4-CH2 OH) 4256-f
Boc-(2S)-(cis/trans)-homoPro(4-CH2CO2 H) 4266-b
Fmoc-(2S)-(cis/trans)-homoPro(4-CH2CO 2H) 4266-f
(2R, 4R) Z-5-Oxazolidinone(2-Ph, 4-Me) 4274-z
Chiral O O N Z
OH
Chiral
OH
Chiral
OH
Chiral
N H
O N O Boc COOH N H
O OMe
(2S, 4S) Z-5-Oxazolidinone(2-Ph, 4-Me) 4276-z
(2R, 4S)-transhomopro(4-OH)-OMe 4284(4R)-oom
Boc-L-cishomoPro(4-hydroxy) 4286-b
L-cishomoPro(4-hydroxy)-OMe 4286-oom
N O S
Chiral Fmoc N H O OH Chiral
H2 N HO
H2 N HO
O HN Fmoc O
NH N OH N H Boc H
1,1-ac-pyran 4296
1,1-ac-thiopyran 4306
Fmoc-L-Trp(5-CN) 4516-f
Boc-L-Trp(5-CH2NH-Fmoc) 4526-bf
Alloc
Boc Chiral NH NH O H O O OH NH NH N Fmoc N Fmoc H H NH Chiral O H O OH Chiral
HN
H N Fmoc HO O Fmoc O
OH
Fmoc-L-Trp(5-CH2NH-Alloc) 4526-fa
Fmoc-L-Trp(5-CH2NH-Boc) 4526-fb
Fmoc-L-Trp(5-COOH) 4536-f
Fmoc-L-Trp(5-CHO) 4546-f
36
O OH N N H H
Chiral
OH HO B Fmoc N H
OH O OH N N H H
Chiral
Chiral
HN HO B HO HN Fmoc COOH
Fmoc
N H
Fmoc
Fmoc-(2R, 3S)-Beta-MeTrp 4554-f
Fmoc-D,L-norTrp 4565-f
Fmoc-L-Trp(5-B(OH)2) 4576-f
Fmoc-L-Trp[2-B(OH)2] 4586-f
Boc HN O
Chiral F F OH N H N H F Fmoc N H H F O OH N Fmoc Chiral HN N N H Fmoc Chiral OH OH O N HN Fmoc O Chiral
Fmoc-L-Trp(5-CH2CH2NH-Boc) 4596-fb
Fmoc-L-Trp(4,5,6,7-tetrafluoro) 4606-f
Fmoc-L-Ala[3-(2-benzimidazoyl)] 4616-f
Fmoc-L-Ala[3-(3-Quinolinyl)] 4626-f
OH NH
Chiral
Chiral OH NH
COOH
Chiral
HO O
NH2Chiral
Fmoc N H N H
N Fmoc H N H
Boc N N H
Fmoc-L-Ala-3-(4-indole) 4636-f
Boc-L-benzoTrp 4646-b
Fmoc-L-benzoTrp 4646-f
L-7-azaTrp 4656
Boc HO O NH
Chiral
Fmoc HO O NH
Chiral
Chiral OH O NH H2N N H
OH
Chiral H N Fmoc
H2 N N H N H
Boc
N H
Boc-L-7-azaTrp 4656-b
Fmoc-L-7-azaTrp 4656-f
Boc-L-Trp(5-NH2) 4666-b
Fmoc-L-Trp(5-NH2) 4666-f
37
O Chiral N Boc OH N Fmoc
O Chiral OH Cl N Fmoc
O Chiral OH
Br N Boc
Chiral COOH
Boc-(2S)-indoline carboxylic acid 4686-b
Fmoc-(2S)-indoline carboxylic acid 4686-f
Fmoc-(2S)-indoline(6-Cl) carboxylic acid 4696-f
Boc-(2S)-indoline(5-Br) carboxylic acid 4706-b
Br N
Chiral COOH Br N Boc Fmoc
Chiral COOH Br N
Chiral COOH Fmoc O
Fmoc H N
Chiral
HO
Fmoc-(2S)-indoline(5-Br) carboxylic acid 4706-f
Boc-(2S)-indoline(6-Br) carboxylic acid 4716-b
Fmoc-(2S)-indoline(6-Br) carboxylic acid 4716-f
Bicyclo-Fmoc-L-Phg-Pro 4806-f
Fmoc H N
Chiral HO
Fmoc H N
Chiral
HO
Fmoc H N
Chiral O Chiral OH Br N Fmoc
O HO O
O HO O
O HO O
Bicyclo-Fmoc-L-Ala-Pro 4816-f
Bicyclo-Fmoc-L-Ser-Pro 4826-f
Bicyclo-Fmoc-L-Thr-Pro 4836-f
Fmoc-L-Tic(7-Br) 4846-f
H Boc N O HO
Chiral Fmoc O
H N O HO
Chiral
H S N O HO O
Chiral
H S HN Fmoc O N HO O
Chiral
N H
N H
HN O Boc
Boc-(3S, 6S, 9S)-Indolizidin-2-one amino acid 4856-b
Fmoc-(3S, 6S, 9S)-Indolizidin-2-one amino acid 4856-f
Bicylco-[6, 5]-Boc-(2S, 3R)-Glu-(2S)-Pen 4956-b
Bicylco-[6, 5]-Fmoc-(2S, 3R)-Glu-(2S)-Pen 4956-f
38
H N Fmoc N H O
Chiral HN Boc OH O O bn
Chiral
Boc O
H N H N Boc
Boc Chiral
HChiral
N Boc H
OH
Fmoc
N H O
OH
Fmoc-L-Dap(Boc) 5006-fb
Z-L-Dap(Boc)-Obn 5006-zbbn
Boc-L-Dab(Boc) 5016-bb
Fmoc-L-Dab(Boc) 5016-fb
Boc Chiral HN O OH Boc Boc NH Chiral O OH H N Fmoc N Boc N Chiral Boc H N Fmoc O OH N H O H
Boc Chiral N H
OH
Boc-L-Orn(Boc) 5026-bb
Fmoc-L-Orn(Boc) 5026-fb
Boc-L-Lys(Boc) 5036-bb
Fmoc-L-Lys(Boc) 5036-fb
OH Boc O S O HN
H N Alloc
H N Boc
H N Alloc
NH3 O
O Fmoc N H
OH Fmoc O N H
OH H2 N O O
OH
L-transLysine(4,5-didehydro, NH-Boc)-OMe, Toluenesulfonic Acid Salt 5036-obm, TSA
Fmoc-D, L-hLys(Alloc) 5045-fa
Fmoc-D, L-hLys(Boc) 5045-fb
D, L-hLys(Alloc) 5045-oa
H N Boc
FmocChiral NH
H N
Chiral Alloc
H N
Chiral Boc
H2 N O
OH
Boc
N H
OH O
Fmoc
N H O
OH
Fmoc
N H O
OH
D, L-hLys(Boc) 5045-ob
Boc-L-hLys(Fmoc) 5046-bf
Fmoc-L-hLys(Alloc) 5046-fa
Fmoc-L-hLys(Boc) 5046-fb
39
Chiral H N Boc Chiral Boc O N Fmoc Fmoc N H OH O N H OH O H2 N O OMe O N Chiral Boc N Chiral
H2N O
OH
L-hLys(Boc) 5046-ob
Fmoc-(2R)-Gly-4Pip(Alloc) 5054-fa
Fmoc-(2R)-Gly-4-Pip(Boc) 5054-fb
(2R)-Gly-4-Pip(Boc)-OMe 5054-obm
Boc N
Chiral
Boc N
Chiral
Boc N
Chiral
Alloc N
H2 N O
OH
N H O
OH
N H O
Fmoc
N H O
OH
(2R)-Gly-4-Pip(Boc) 5054-obo
Z-(2R)-Gly-4-Pip(Boc) 5054-zb
Z-(2R)-Gly-4-Pip(Boc)-OMe 5054-zbm
Fmoc-(2S, 2R)-Gly-4Pip(Alloc) 5055-fa
Boc N
Boc N
Chiral
Z N
Chiral
Alloc N
Chiral
Fmoc
N H O
OH
Boc
N H
OH O
Boc
N H O
OH
Fmoc
N H O
OH
Fmoc-(2S, 2R)-Gly-4-Pip(Boc) 5055-fb
Boc-(2S)-Gly-4Pip-Boc 5056-bb
Boc-(2S)-Gly-4Pip-Z 5056-bz
Fmoc-(2S)-Gly-4Pip(Alloc) 5056-fa
Boc N
Chiral
Alloc N
Chiral
Boc N
Chiral
Boc N
Chiral
Fmoc
N H O
OH
H2N O
OH
H2 N O
N H O
Fmoc-(2S)-Gly-4Pip(Boc) 5056-fb
(2S)-Gly-4Pip(Alloc) 5056-oa
(2S)-Gly-4-Pip(boc)-OMe 5056-obm
Z-(2S)-Gly-4-Pip(Boc)-OMe 5056-zbm
40
AllocChiral N N
AllocChiral N
Boc N
BocChiral
OH Fmoc N H Fmoc O N H
OH Fmoc O N H O OH HN Boc
OH O
Fmoc-D-Ala-4Pip(Alloc) 5064-fa
Fmoc-D, L-Ala-4Pip(Alloc) 5065-fa
Fmoc-D, L-Ala-4Pip(Boc) 5065-fb
Boc-L-Ala-4Pip(Boc) 5066-bb
AllocChiral N
BocChiral N N
AllocChiral
BocChiral N
OH O H2 N O
OH H2 N
O O
Fmoc-L-Ala-4Pip(Alloc) 5066-fa
Fmoc-L-Ala-4Pip(Boc) 5066-fb
L-Ala-4Pip(Alloc) 5066-oa
L-Ala-4Pip(Boc)-OMe 5066-obm
H N Alloc
H N Boc
H N
Chiral Alloc
Chiral N Boc
OH Fmoc O N H O
OH Fmoc N H
OH O
Fmoc-D,L-cis/trans-Cha(4-NH-Alloc) 5075-fa(c/t)
Fmoc-D, L-cis/trans-Cha(4-NH-Boc) 5075-fb(c/t)
Fmoc-L-cis/trans-Cha(4-NH-Alloc) 5076-fa(c/t)
Fmoc-L-cis/trans-Cha(4-NH-Boc) 5076-fb(c/t)
Chiral N Alloc
Alloc
N H
Chiral
Boc
N H
Chiral
Alloc
N H
OH H2 N O
H N Fmoc O
OH
H N Fmoc O
OH
H N Fmoc O
OH
L-cis/trans-Cha(4-NH-Alloc) 5076-oa(c/t)
Fmoc-D-Ala(3-pyrrolidinyl-(2-N-Alloc) 5084-fa
Fmoc-D-Ala(3-pyrrolidinyl-(2-N-Boc) 5084-fb
Fmoc-D, L-Ala(3-pyrrolidinyl-(2-N-Alloc) 5085-fa
41
Boc
N H
Alloc
N H
Chiral
Boc
N H
Chiral
Alloc
N H
Chiral
H N Fmoc O
OH
H N Fmoc O
OH
N Fmoc O
OH
H2N O
OH
Fmoc-D, L-Ala(3-pyrrolidinyl-(2-N-Boc) 5085-fb
Fmoc-L-Ala(3-pyrolidinyl-(2-N-Alloc) 5086-fa
Fmoc-L-Ala(3-pyrolidinyl-(2-N-Boc) 5086-fb
L-Ala(3-pyrolidinyl-(2-N-alloc) 5086-oa
Boc NH HN H Tfa N H O Fmoc N H Chiral Fmoc N O H O OH N Alloc H OH O H O Fmoc N OH N Alloc H Chiral
Tfa-L-Ala[3-(2S)pyrrolidinyl (N-H)]-OMe 5086-tm
Fmoc-D, L-trans-Cha(4-CH2NH-Alloc) 5095-fa
Fmoc-D, L-trans-Cha(4-CH2NH-Boc) 5095-fb
Fmoc-L-trans-Cha(4-CH2NH-Alloc) 5096-fa
AllocChiral Chiral N H O OH N Boc H OH O N H NH O O N Boc H Fmoc ClH Chiral
Alloc N
Fmoc
N H O
OH
H2N
Fmoc-L-trans-Cha(4-CH2NH-Boc) 5096-fb
L-trans-Cha(4-CH2NH-Alloc) 5096-oa
L-trans-Cha(4-CH2NH-Boc)-HCl 5096-obm
Fmoc-D, L-homo[Ala-4-Pip(N-Alloc)] 5105-fa
Boc N
Boc N
Chiral
Alloc N
Chiral
Boc N
Chiral
Fmoc
N H O
OH
Boc
N H
OH O
Fmoc
N H O
OH
Fmoc
N H O
OH
Fmoc-D, L-homo[Ala-4-Pip(N-Boc)] 5105-fb
Boc-L-homo[Ala-4-Pip(N-Boc)] 5106-bb
Fmoc-L-homo[Ala-4-Pip(N-Alloc)] 5106-fa
Fmoc-L-homo[Ala-4-Pip(N-Boc)] 5106-fb
42
Alloc N
Chiral N N Fmoc N H OH O Fmoc N H BocChiral
Boc NH Chiral
Fmoc NH
Chiral O
H2 N O
OH
OH O
N Boc
OH
L-homo[Ala-4-Pip(N-Boc)] 5106-oa
Fmoc-L-Ala[3-(1-N-piperazinyl(4-N-Boc) )] 5116-fb
Fmoc-(2S)-diamino(8-N-Boc)octanoic acid 5126-fb
Fmoc-(2S, 3R)-Gly-3-Pip(Boc) 5136(3R)-fb
Fmoc NH
Chiral O
HN
Boc Chiral
Fmoc O HN
FmocChiral OH NH N HO O
N Boc
OH Fmoc N H O OH N Boc
Boc
Fmoc-(2S, 3S)-Gly-3-Pip(Boc) 5136(3S)-fb
Fmoc-(2S)-trans-Chg(4-NH-Boc) 5146-fb
Fmoc-[(2S, 3S), (2S, 3R), (2R, 3S), (2R, 3R)]-Ala-3-Pip(Boc) 5155-fb
Fmoc-(2S, 3S)-Ala-3-Pip(Boc) 5156(S)-fb
FmocChiral NH N Boc HO O
Fmoc N OH O
Alloc N OH O
Boc N OH O
Boc
N H
Fmoc
N H
Fmoc
N H
Fmoc-(2S, 3R)-Ala-3-Pip(Boc) 5166(R)-fb
Boc-4,4-acp(1-N-Fmoc) 5173-bf
Fmoc-4,4-acp(1-N-Alloc) 5173-fa
Fmoc-4,4-acp(1-N-Boc) 5173-fb
Boc N O O
Boc N OH O
Z N OH O
HO O
Chiral OH
NH Fmoc Boc NH
H2 N
H2N
H2 N
4,4-acp(1-N-Boc)-OMe 5173-obm
4,4-acp(1-N-Boc) 5173-obo
4,4-acp(1-N-Z) 5173-ozo
Boc-(2S, 5S)-Lysine(5-OH, N-Fmoc) 5176(5S)-bf
43
OH O Alloc NH Fmoc NH
Fmoc Chiral HO O OH OH NH Boc Fmoc NH Boc N H OH O Fmoc Chiral NH
HN Alloc
N H
OH O
Fmoc-(2S, 5S)-Lysine(5-OH, N-Alloc) 5176(5S)-fa
Fmoc-(2S, 5S)-Lysine(5-OH, N-Boc) 5176(5S)-fb
Boc-(4-cis/trans)-1, 1-acch(4-amino-Fmoc) 5183-bf
Fmoc-1, 1-acch(4-amino-Alloc) 5183-fa
HN Boc
HN Boc N H
FmocChiral N H OH
AllocChiral
Fmoc
N H
OH O
H2 N O
O Boc N H O
OH
HN Fmoc O
Fmoc-1, 1-acch(4-amino-Boc) 5183-fb
1, 1-acch(4-amino-Boc)-OMe 5183-om
Boc-L-Ala[3-(3S)Pyrrolidinyl(Fmloc)] 5196-bf
Fmoc-L-Ala[3-(3S)Pyrrolidinyl(Alloc)] 5196-fa
BocChiral N H OH H O N
BocChiral
H N
Fmoc
H N Alloc
HN Fmoc O
H2 N O
Boc
N H
O OH
Fmoc
N H
O OH
Fmoc-L-Ala[3-(3S)Pyrrolidinyl(Boc)] 5196-fb
L-Ala[3-(3S)Pyrrolidinyl(Boc)]-OMe 5196-obm
Boc-(4-cis/trans)-1, 1-acch(4-CH2-NH-Fmoc) 5203-bf
Fmoc-(4-cis/trans)-1, 1-acch(4-CH2-NH-Alloc) 5203-fa
H N Boc
H N Boc
HN
Fmoc
Chiral
HN
Alloc
Chiral
N Fmoc N H O OH H2 N O O
O OH
O OH
HN
Boc
HN
Fmoc
Fmoc-(4-cis/trans)-1, 1-acch(4-CH2-NH-Boc) 5203-fb
(4-cis/trans)-1, 1-acch(4-CH2-NH-Boc)-OMe 5203-obm
Fmoc-L-Ala-3[1N-(4-NH-Boc)piperidine 5216-bf
Fmoc-L-Ala-3[1N-(4-NH-Alloc)piperidin e 5216-fa
44
HN
Boc
Chiral O
tBuChiral O O
OH Chiral
OH Chiral tBu
O OH Fmoc N H O OH Boc N H
O Boc O N H
O O
HN
Fmoc
Fmoc-L-Ala-3[1N-(4-NH-Boc)piperidine 5216-fb
Fmoc-D-Glu(OtBu)-OH 5504-fou
Boc-L-Glu-OMe 5506-bom
Boc-L-Glu-OtBu 5506-bou
tBuChiral O O OH H2 N O OH HO B HO O NH Boc Chiral
OH Chiral HO OH B O N Fmoc H
Boc
N H
OH O
HO
L-Glu(OtBu)-OH 5506-ouo
Boc-L-pentenoic[5-B(OH)2] acid 5516-b
Boc-(2S, 3S)-Glu(3-Me) 5516-boo
Fmoc-L-pentenoic[5-B(OH)2] acid 5516-f
OH Chiral HO OH B O N Boc H
HO
OH Chiral HO
OH B
Chiral
Fmoc
N H
OH O
HO
HO O
Boc
Fmoc
N H
OH O
Fmoc-(2S, 3S)-Glu(3-Me) 5516-foo
Boc-L-pentanoic[5-B(OH)2] acid 5526-b
Boc-(2S, 3R)-Glu[3-(4-hydroxyphenyl)] 5526-booo
Fmoc-L-pentanoic[5-B(OH)2] acid 5526-f
HO
OH Chiral HN HO Boc O Chiral HO O O HN Fmoc Chiral O O N Boc O Chiral OH
HO O
N Fmoc H
Fmoc-(2S, 3R)-Glu[3-(4-hydroxyphenyl)] 5526-fooo
Boc-(2S)-aminopentanoic acid-4-one 5536-b
Fmoc-(2S)-aminopentanoic acid-4-one 5536-f
Boc-(2S, 3S)-Pyroglut(3-Me) 5546-b
45
Chiral O N Boc O tBuChiral O
Boc O
H N O O tBu
Chiral
Boc O
H N O O tBu
Chiral
O N Boc O
F OH
Cl
Cl
Boc-(2S, 3S)-Pyroglut(3-CF3) 5556-b
Boc-(2S)-Pyroglut-tBu 5566-bu
Boc-D-Glu(5-CH2-Cl)-OtBu 5574-bu
Boc-L-Glu(5-CH2-Cl)-OtBu 5576-bu
Chiral O
Chiral O O O HN Tfa O OChiral Boc N Boc O O O O Chiral
Boc
N Boc O
Boc
N Boc O
Boc2-D-Glu(5-OMe)-OMe 5584-b2mm
Boc2-L-Glu(5-OMe)-OMe 5586-b2mm
Tfa-L-Aspartic Acid Anhydride 5586-tf
Boc2-D-Asp(OMe) 5594-b2mm
Chiral O O Boc N Boc O O O N Boc O OH O N H O O O OH Chiral OH Chiral O H N Fmoc HN N
PMC NH H
Boc2-L-Asp(OMe) 5596-b2mm
Boc-(2S, 3R)-Pyroglut[3-(4-hydroxyphenyl)] 5606-b
(2S, 3R)-Pyroglut[3-(4-hydroxyphenyl)-O-Bn]OBn 5606-obnbn
Fmoc-D, L-Phe[4-Guanido-Pmc] 6005-fp
PMCChiral PMCChiral HN H O OH N Fmoc N NH H O OH NH2 HN N PMCChiral NH H OH Fmoc N H O Fmoc N H O OH H HN N N H Chiral Pmc HN N NH
Fmoc-L-Phe[4-Guanido-Pmc] 6006-fp
L-Phe[4-Guanido-Pmc] 6006-op
Fmoc-L-norArg(Pmc) 6016-fp
Fmoc-(R)-Gly-4-Pip[N-Amidino(Pmc)] 6064-fp
46
PMC HN N NH HN N
PMCChiral NH HN N
Pmc Chiral NH HN N
Pmc Chiral NH
Fmoc
N H O
OH
Fmoc
N H O
OH
H H N Ac- O
H2 N O
OH
Fmoc-(R, S)-Gly-4-Pip[N-Amidino(Pmc)] 6065-fp
Fmoc-(S)-Gly-4-Pip[N-Amidino(Pmc)] 6066-fp
(S)-Gly-4-Pip[N-Amidino(Pmc)]-OMe-Ac etate Salt 6066-omp
(S)-Gly-4-Pip[N-Amidino(Pmc)] 6066-op
Chiral Boc N N N H HN N HN
Pmc Chiral
N N
NH2
N N
NH2
H Fmoc N H O OH H N FmocO
OH
Boc
N H O
OH
Fmoc
N H O
OH
Fmoc-L-Orn[2-(1N-Boc)4, 5-dihydroImidazole] 6076-fb
Fmoc-L-Ala[3-(2S)-pyrrolidinyl(2-N-amidino(Pmc)] 6086-fp
Boc-(R, S)-2-amino-4-[(2-amino)pyrimidinyl]buta noic acid 6095-b
Fmoc-(R, S)-2-amino-4-[(2-amino)pyrimidinyl]buta noic acid 6095-f
N N
NH2
Chiral
N N
NH2 Chiral
N N
NH2 Chiral
HN N N H PMC
H2 N O
OH
Boc
N H O
OH
Fmoc
N H O
OH
OH Fmoc N H O
(S)-2-amino-4-[(2-amino)pyrimidinyl]buta noic acid 6096
Boc-(S)-2-amino-4-[(2-amino)pyrimidinyl ]butanoic acid 6096-b
Fmoc-(S)-2-amino-4-[(2-amino)pyrimidin yl]butanoic acid 6096-f
Fmoc-D, L-Ala-4-Pip[(N-amidino-Pmc)] 6115-fp
HN N H N
Chiral PMC
HN N
Chiral N PMC H
HN N NH
Chiral NH Chiral HN O Boc IH OH NH2
PMC
OH Fmoc N H O H2 N
OH O H2 N
O O
Fmoc-L-Ala-4-Pip(N-amidino-Pmc) 6116-fp
L-Ala-4-Pip(N-amidino-Pmc) 6116-op
L-Ala-4-Pip(N-amidino-Pmc)-OMe 6116-opm
Boc-L-Phe(4-amidino) HI Salt 6126-b
47
NH HN O OH Boc N H
Chiral Alloc
NH Fmoc O OH N H N H
Chiral Alloc O
NH NH2 N H OH
Chiral Alloc O
ClH NH2 ClH O
NH
Chiral
NH2
Boc-L-Phe(4-amidino-Alloc) 6126-ba
Fmoc-L-Phe(4-amidino-Alloc) 6126-fa
L-Phe(4-amidino-Alloc) 6126-oa
L-Phe(4-amidino)-OMe 2HCl 6126-oom
HN Fmoc H N O N H OH NH N Pmc H Fmoc N H Chiral N
PMC NH
HN N
PMC Chiral NH
HN N
PMC Chiral NH
OH O
Fmoc
N H
OH O H2 N O
OH
Fmoc-L-Ala(3-guanido-Pmc) 6136-fp
Fmoc-D, L-homo-[Ala-4-Pip(N-amidino(Pmc)] 6145-fp
Fmoc-L-homo-[Ala-4-Pip(N-amidino(Pmc )] 6146-fp
L-homo-[Ala-4-Pip(N-amidino(Pmc)] 6146-op
HN HN H O OH N Fmoc
PmcChiral NH
HN
Mtr Chiral NH NH
HN
Pbf Chiral NH NH
HN
Pmc Chiral NH NH
OH Fmoc N H O Fmoc N H
OH OH O Fmoc N H O
Fmoc-L-Phe[4-CH2-(guanidino-(Pmc))] 6156-fp
Fmoc-L-Arg(Mtr) 6166-fmr
Fmoc-L-Arg(Pbf) 6166-fpb
Fmoc-L-BishomoArg(Pmc) 6176-fp
NH H Pmc N HN N Fmoc OH O Fmoc N H H N Chiral HN NH Pmc
Chiral Fmoc N H O N OH O HN NH PMC OH
Chiral Fmoc NH O N HN NH PMC OH
Chiral
Fmoc-L-transPro[4-guanidino-(Pmc)] 6186-fp
Fmoc-L-Phg(4-guanidino-Pmc) 6196-fp
Fmoc-(2S,3R)-Gly-3-Pip[N-amidino-(Pmc )] 6206(R)-fp
Fmoc-(2S, 3S)-Gly-3-Pip[N-amidino-(Pmc)] 6206(S)-fp
48
NH HN NH Pmc
Chiral Pmc
H N
NH Chiral NH
N NH
Chiral HN N
PMC NH
H Fmoc N H OH O O
Fmoc H Fmoc N O OH
Alloc Fmoc N H
OH O
OH
Fmoc-(2S)-transChg[(4-guanidino(Pmc)] 6216-fp
Fmoc-L-Phe[3-CH2-(guanidino-(Pmc))] 6226-fp
Fmoc-L-Phe[4-(2-(3-N-Alloc)4, 5-dihydroimidazole)] 6236-fa
Fmoc-4,4-acp(1-N-amidino-Pmc) 6246-fp
Pmc HN NH N
Chiral
Pmc
H N N N
NH
Chiral
Pmc
H N
NH NH HN
NH
Chiral
N PMC H
O OH Fmoc N H O OH N COOH Fmoc
O N Fmoc OH
HN
Fmoc
Fmoc-(2S)-Piperizine (4-N-amidino-Pmc) 6256-fp
Fmoc-L-Ala-3-(N-Piperazine-4-N-amidin o-Pmc) 6266-fp
Fmoc-(4-cis/trans)-1, 1-acch(4-guanidino-Pmc) 6273-fp
Fmoc-L-transhomoPro(4-N-amidino-Pmc) 6286-fp
NH HN N PMC H O O
Chiral Boc H N O Chiral OH OH O O Chiral O N Trityl H O H N Chiral
N H
Trityl
L-transhomoPro(4-N-amidino-Pmc)-OMe 6286-opm
Boc-L-Ser(3,3-dimethyl) 6506-b
Trityl-D-Ser-lactone 6514-t
Trityl-L-Ser-lactone 6516-t
O HO HN Boc
Chiral OH Boc N H
Chiral OMe Boc N H
Chiral OMe O
Ts O O Boc N H O
Chiral
Boc-L-Ser 6526-b
Boc-D-Ala(3-I)-OMe 7504-bm
Boc-L-Ala(3-I)-OMe 7506-bm
Boc-D-Ser(OTs)-OMe 7514-bOTsm
49
Ts O O Boc N H O
Chiral
Cl H2 N O
Chiral OH H2 N
Cl OH
Chiral Boc N H
Cl
Chiral OH
Boc-L-Ser(OTs)-OMe 7516-bOTsm
D-Ala-3-Cl 7524
L-Ala-3-Cl 7526
Boc-L-Ala(3-Cl) 7526-b
Chiral
Chiral O O OH O Boc N H
Chiral Boc OH O
H N O
O NH
Chiral
O OH Boc N H O Fmoc N H
OH Fmoc N H O
Boc-L-Ser(O-Allyl)-OH 7536-ball
Fmoc-L-Ser(O-Allyl)-OH 7536-fall
Boc-L-Thr(CH2CHCH2) 7586-ball
Fmoc-L-DAP(Boc-Aoa) 7596-fb
Chiral O O HN Boc OH O Fmoc N H O OH
Chiral
Boc NH O OH
Chiral Cl O OH
Boc NH
Chiral Cl
Boc-(2S)-CHG(4-oxo) 7606-b
Fmoc-(2S)-CHG(4-oxo) 7606-f
[(2R)-4-chlorobenzyl]-N-Boc-3-aminopro pionic acid 8504-b
[(2S)-4-chlorobenzyl]-N-Boc-3-aminoprop ionic acid 8506-b
ClChiral
O N
COOH
Boc
N H
OH O O O O N H OH
O OH
Br
N -(t-butoxycarbonyl)-methyl-4-chloro-D-phenylalanine 8514-b
Boc-(3S, 3R)-3-amino-[3-(4-pip(Boc)]propionic acid 8525-bb
4-Acetyl-3,5-dioxo-Cha(1-Me, 1-COOH) 9003
1-Benzyloxy-2-bromoethane 9013
50
Cl F OH OH F Cl OH N S
CN Cl
Cl N P Cl
1,2-Bis(hydroxymethyl)-4-fluorobenzene 9023
1-Chloromethyl-2-hydroxymethyl-4-fluoro benzene 9033
3,5-Dichloro-4-cyano-isothiazole 9043
Diethylphosphoramidous dichloride 9053
Chiral OH NH2 HO O
HN O S N H O
O O O
O O N
1-Cyclopropyl-prop-2-en-ol 9063
L-Bip-ol 9076
Pmc-Mit 9083-p
Alloc-O-Su 9093
OH Chiral
OH Chiral Chiral N H Boc CN N H Boc Chiral COOH
N Boc
N Boc
N-Boc-(3R)-Pip(3-CH2OH) 9104-b
N-Boc-(3S)-Pip(3-CH2OH) 9106-b
N-Boc-(2S)-Pyrr(2-CHCN) 9116-b
N-Boc-(2S)-Pyrr(2-CHCOOH) 9126-b
CNChiral
CNChiral
COOHChiral
COOHChiral
N Boc
N Boc
N Boc
N Boc
N-Boc-(3R)-Pip(3-CH2CN) 9134-b
N-Boc-(3S)-Pip(3-CH2CN) 9136-b
N-Boc-(3R)-Pip(3-CH2COOH) 9144-b
N-Boc-(3S)-Pip(3-CH2COOH) 9146-b
51
O O O S O I
HO
N B
TIPS NH Boc NH Boc HN Boc
HO
3-B(OH)2-Indole(N-TIPS) 9153-TIPS
Boc-4-aminocyclohexanone 9163
Boc-aminocyclohexane-4-ms 9173-bms
Boc-aminocyclohexane-4-Iodomethyl 9183-b
HO
Chiral
OH O
2S-Mdp 9186
52
53
54

RSP 601

Hochgeladen von

Dokumentinformationen

Originaltitel

Copyright

Verfügbare Formate

Dieses Dokument teilen

Dokument teilen oder einbetten

Freigabeoptionen

Stufen Sie dieses Dokument als nützlich ein?

Sind diese Inhalte unangemessen?

Copyright:

Verfügbare Formate

RSP 601

Hochgeladen von

Copyright:

Verfügbare Formate

RSP Amino Acids, LLC 2007-2008 Building Block Index Structural Index, Version 6.

RSPs Structural Index, Version 6.01 for 2007-2008

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Warranties Cancellations Index by RSP Number

Amino Acid Building Blocks and Scaffolds

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

RSP number abbreviations for analogue protection

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Building Blocks and Scaffolds

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Chiral Chiral Z N H O OH NH2 O ClH O OH Boc N H O Boc N H O O

Z-D-2-Aminobutyric Acid 0014-Z

Boc-(2R)-2-amino-5-hexenoic acid 0034-b

Boc-(2R)-2-amino-5-hexenoic acid, methylester 0034-bm

(2S)-2-amino-5-hexenoic acid 0036

(2S)-Boc-2-amino-5-hexenoic acid 0036-b

(2S)-Boc-2-amino-5-hexenoic acid methylester 0036-bm

(2S)-Fmoc-2-amino-5-hexenoic acid 0036-f

(2S)-2-amino-6-heptenoic acid 0046

(2S)-Boc-2-amino-6-heptenoic acid 0046-b

(2S)-Fmoc-2-amino-6-heptenoic acid 0046-f

(2S)-2-amino-7-octenoic acid 0056

(2S)-Boc-2-amino-7-octenoic acid 0056-b

(2S)-Fmoc-2-amino-7-octenoic acid 0056-f

(2S)-Boc-2-amino-8-nonenoic acid 0066-b

(2S)-Fmoc-2-amino-8-nonenoic acid 0066-f

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Chiral Chiral HO O N Boc H H2 N O O Boc Chiral OH O O O Chiral

Boc-(2S)-2 amino-9-decenoic acid 0076-b

Boc-1, 1-accp 0093-b

Fmoc-1, 1-accp 0093-f

Boc-1, 1-accb 0103-b

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Bp-Gly-OtBu Schiff Base 0116-Bpu

Boc-(2R, 2S)-Gly[PO(OMe)2]-OMe 0126-Bmm

Bp-(2R, 2S)-Gly(2-OAc)-OMe 0136-Bpam

Chiral OH H2 N O N Boc N H O Chiral O O HN Z O O O HN Boc OH O

(1S, 2S)-pseudoephedrine glycinamide 0156

Boc-(2R, 2S)-Gly(2-OMe)-OMe 0165-bmm

Z-(2R, 2S)-Gly(2-OMe)-OMe 0165-zmm

Chiral OH HN Fmoc O H2N

Chiral OH HN Fmoc O H2N

Phone: 978-448-3911, Fax: 978-448-2914 rsp@amino-acids.com, www.amino-acids.com

RSPs Structural Index, Version 6.01 for 2007-2008

Chiral O H H NH2 COOH H H Boc N H O OH

(2R, 2S)-Gly[2-cyclohexyl(4-oxo, full Et-ketal)-OMe 0196-oacm

Z-(2R, 2S)-Gly[2-cyclohexyl(4-oxo, full Et-ketal)-OMe 0196-zacm

Boc-(2S)-2-amino-heptanoic acid 0216-b

Fmoc-D, L-norTyr(tBu) 1015-fu