Rpa131400244014

174 | P a g e
International Standard Serial Number (ISSN): 2319-8141

International Journal of Universal Pharmacy and Bio Sciences 2(6): November-December 2013
INTERNATIONAL JOURNAL OF UNIVERSAL

PHARMACY AND BIO SCIENCES
IMPACT FACTOR 1.89***

ICV 2.40***
REVIEW ARTICLE!!!
Pharmaceutical Sciences
VALUABLE INSIGHT INTO THE SYNTHESIS AND BIOLOGICAL

ACTIVITIES OF FUSED HETEROCYCLIC NUCLEUS USING
MICROWAVE
Anshul Chawla, Harmanjit Kaur
CT Institute of Pharmaceutical Sciences, Shahpur, Jalandhar-144020 (Punjab) INDIA.
KEYWORDS:
Fused Heterocyclic
Compounds, Biological
activities, Irradiation,
ABSTRACT
In this paper the importance of microwave assisted synthesis of
fused heterocyclic compounds has been discussed extensively.
Microwave assisted organic synthesis is an enabling technology for
Synthesis.
For Correspondence:
drug development process. Since the last few years, high speed
Anshul Chawla *
microwave synthesis is being practiced owing to its vitality in
Address:
Asst. Professor
organic synthesis procedures. It is very well known to all of us that
Pharmaceutical chemistry
the heterocyclic compounds play a vital role in medicine,
CT Institute of
displaying
Pharmaceutical Sciences,
antimicrobial,
Shahpur, Jalandhar
(Punjab)-144020.
broad
spectrum
cytotoxic
antimycobacterial,
of
to
biological
tumor
anticonvulsant,
activities
cells,
like
anticancer,
anti-inflammatory,
cardiovascular, antioxidant, anti-inflammatory, anti-HIV activities

etc. This review is summarized to discuss the most active fused
heterocyclic compounds synthesis via microwave irradiations.
Full Text Available On www.ijupbs.com
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INTRODUCTION:
Conventional thermal heating suffers from common limitations such as drastic reaction
conditions,
time consuming, excessive use of solvent and several side reactions. Rapid expansion and popularity
of assisting a wide range of organic reactions by exposure to microwave have been accompanied by
achieving reactions under solvent-free conditions, reducing reaction times, and increasing the yield
of products and even selectivity. Moreover, in addition to the economic impact, there are additional
advantages such as the use of noncorrosive, inexpensive, and environment friendly catalysts, thus
leading to eco-friendly approaches known as green chemistry, in comparison with their
conventional thermal heating counterpart. [1]
Some publications recognize the twelve principles of green chemistry, like prevention, atom
economy, less hazardous chemical synthesis, designing safer chemicals, safer solvents and
auxiliaries, design for energy efficiency, use of renewable feedstocks reduce derivatives, catalysis,
design for degradation, real-time analysis for pollution prevention, inherently safer chemistry for
accident prevention. [2] As anyone who has ever spilled the contents of a food container onto the
floor well knows, it is better to not make a mess than to clean it up once made. As applied to green
chemistry, this basic rule means that waste prevention is much better than waste cleanup. Failure to
follow this simple rule has resulted in most of the
troublesome hazardous waste sites that are
causing problems throughout the world today. One of the most effective ways to prevent generation
of wastes is to make sure that insofar as possible all materials involved in making a product should
be incorporated into the final product. Therefore, the practice of green chemistry is largely about
incorporation of all raw materials into the product, if at all possible. The practice of green chemistry
is making substantial progress in designing chemicals and new approaches to the use of chemicals
such that effectiveness is retained and even enhanced while toxicity is reduced. [3] This section
addresses the main ones of these. The growing number of publications in microwave-assisted
synthesis includes virtually all types of chemical reactions such as additions, cycloadditions,
substitutions, eliminations, fragmentations etc. All these have attracted our attention to review the
available literature on the role of microwaves in the field of heterocyclic chemistry, bearing in mind
that most biologically active compounds are heterocyclics. Heterocycles have either fused benzene
or other heterocyclic rings. The fused heterocyclic compounds are located according to the
heterocycle that was built under microwave irradiation or as a reaction of these heterocyclics acting
as precursors. [4] In the present review, we are trying to highlight some of the applications of
microwave methodology in heterocyclic chemistry. Fused heterocyclic compounds are reviewed by
presenting their methods of preparation of the desired ring, through microwaves. As their biological
actions such as antimicrobial activity through DNA gyrase-B, antioxidant activity against
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superoxide and hydroxyl radicals, antimicrobial activity against E. coli and S. aureus, antibiotic and
cytotoxic activities, anti-inflammatory, antiaging, and anticancer activity, potent nonpeptidic
inhibitors of HIV protease. They exhibit a broad range of biological activities including
anticoagulation, antifungal, anti-psoriasis etc. [5] Undoubtedly, microwaves are going to be highly
important in future synthesis of heterocyclic compounds.
Nomenclature of the fused ring system:
As the present review deals with the synthesis of heterocyclic fused ring systems, its nomenclature
is herewith shortly discussed. The nomenclature follows the following rules:
1) The individual components are named without any application of fused ring system.
2) The parent component is represented in the fusion name by citing it last in the name. The parent
component is the one with highest priority according to the following criteria:
a) A heterocyclic component containing the heteroatom occurring earliest in the order: N,
F, Cl, Br, I, O, S, Se, Te, P, As, Sb, Bi, Si, Ge, Sn, Pb, B, Hg.
b) A component containing the larger ring.
c) A component containing the greater number of heteroatoms.
d) A component containing the greater variety of heteroatoms.
3) The attached component is then added as a prefix to the parent component. In the name of
the prefix, the terminal 'e' is changed to 'o'.
4) The bonds of the parent component are indicated by a,b,c...starting with the bond normally
occupying the 1,2 positions. The atoms of the attached component are numbered as usual,
following the order of numbers in the original heterocycle.
5) The numbering of the final condensed heterocycle is carried out independently, starting at
an atom adjacent to a bridged-head atom, whereby heteroatoms receive the smallest possible
number. [6]
Evolution of Some Heterocyclic Compounds:
All most all the heterocyclic compounds have most potent pharmacological activities, some of them
are reported here as important heterocyclic compounds viz sulfa drugs (1933, as first antibacterial
drug), penicillin (1940, as antibiotics), chloroquine (1945, as antimalarial), methyldopa (1950, as
antidiabetic), chlorthiazide (1957, as diuretic), adrenergic -blocker (1958, as coronary vasodilator),
semi synthetic penicillins (1960, as antibacterial), trimethoprim (1965, as antimicrobial), disodium
chromoglycoate (1967, as antiallergic). [7]
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Classification of fused heterocyclic compounds:

Classification of fused heterocyclic compounds
Compounds
without N,O,S
Compounds with
nitrogen
With
1N
With
2N
With
4N
Compounds with
oxygen
With
1O
Compounds with Compounds

one sulphur
with N,O
Compounds with
N,S
With
2O
I) Compounds without N,O,S :
a) Naphthalene
b) Anthracene
c) Coronene
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II) (i) Compounds with one nitrogen:
a) Quinoline
N
b) Indole
c) Isoindole
NH
N
H
d) Acridine
H
N
e) Azepine
N
g) Carbazole
f) Pyrrole
N
H
h) Quinoxaline
N
N
(ii) Compounds with two nitrogens :
b) Indazole
a) Pyrazole
N
H
c) Imidazole
N
N
H
d) Quinazoline
N
H
e) Benzimidazole
H
N
N
(iii) Compounds with 4 nitrogens :
N
a) Purine
N
N
b) Pteridine
N
N
H
N
N
N
N
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III) (i) Compounds with one oxygen:
a) Benzofuran
O
c) Xanthene
b) Chromene
O
(ii) Compounds with 2 oxygen:
a) Coumarin
O
IV) Compounds with sulphur:
a) Benzothiophene
S
a) Benzoxazole
V) Compounds with N,O
N
O
a) Benzothiazole
VI) Compounds with N,S
N
S
Microwave Assisted Synthesis of Heterocyclic Compounds:

Heterocyclic scaffolds represent the central framework of many biologically active compounds.
Microwave is one of the potential green chemistry technique used the recent years. The ability of
microwave-assisted organic synthesis to rapidly synthesize organic compounds is of significant
benefit for library generation. Moreover, it allows modifications in selectivity (chemo, regio, and
stereo-selectivity) and solvent, catalyst-free conditions. This review outlines the use of microwave,
highlights the importance of a number of heterocycles, and summarizes some advances in their
synthesis under microwave irradiation. The synthesis of fused heterocyclics via microwave is given
below:
I a) Naphthalene Derivatives: Naphthalene is an organic compound with formula C10H8. It is the
simplest polycyclic aromatic hydrocarbon, and is a white crystalline solid with a characteristic
odour. As an aromatic hydrocarbon, naphthalene's structure consists of a fused pair of benzene rings.
1. Aminonaphthalene: 2 g of the hydroxyl aromatic compound, 0.024 mol of amine and 10 to 12
ml of a freshly prepared aqueous solution of 0.024mol of amine (equivalent quantities of aqueous
ammonia or 40% aqueous dimethylamine were used in the synthesis of amine or dimethylamine
derivatives,
respectively)
saturated with
sulfur
dioxide were introduced in
a sealed
poly(tetrafluoroethylene) acid digestion vessel and irradiated in microwave for 30 min at 150 Watts
(23% of energy efficiency). [8]
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OH NH ,(NH ) SO
3
4 2
3
NH2
H2O, 150OC
(1)
(2)
2. 2,2'-[Naphthalene-2,7-diylbis(oxy)]bis[N'-substituted acetohydrazide](6): Mix 2,2'-(naphthalene

-2,7-diylbis(oxy)) diacetohydrazide (5) (0.01 mol), aryl / hetero aromatic aldehyde (0.02 mol) and
catalytic amount of glacial acetic acid were taken in DMSO (2 mL) in a beaker and then the reaction
mixture was subjected to microwave irradiation for the interval of 1 min at 180 W. [9]
HO
OH
+
O
Cl
K2CO3
dry IMF, 800C
O
O
(3)
(4)
NH2NH2H2O
O
N
H
O
O
N
H
O
R - CHO H N
2
R
HN
H+, MW
O
O
N
H
NH2
(5)
(6)
Synthetic pathway for the preparation of compounds (6)

b) Anthracene derivatives: Anthracene is a solid polycyclic aromatic hydrocarbon consisting of
three fused benzene rings. It is a component of coal tar. Anthracene is used in the production of the
red dye alizarin and other dyes. Anthracene is colorless but exhibits a blue (400-500 nm peak)
fluorescence under ultraviolet light.
1.
9, 10-dihydro-9,10-ethanoanthracene-11- carboxylic acid methyl ester: A mixture of
anthracene (7) and methyl acrylate (8 ) in xylene (an excellent energy transfer medium) was
irradiated (1000 W) in a microwave oven for 6-8 min, compound (9) was obtained in 70-85% yield.
[10]
6-8 min
MW Irrad.
+
CO2Me
(8)
(7)
24 hr
sealed tube
48 hr
reflux
CO2Me
70-85%
81%
84%
(9)
2. 9- Haloanthracene: Place a nucleophile and an aryl halide (0.1 mmol) in an appropriate solvent
(NMP or DMSO, 1 ml) in a reaction vessel (12 ml). A base [t-BuOK or CsOH (1.1 equiv vs
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nucleophile)] or CuI (as indicated in the text) could be added to enhance the reactivity. The reaction
vessel was then placed in microwave reactor and irradiated. [11]
R
Nucleophile, solvent
Microwave
(11)
(10)
Reactions of 9-halophenanthrene with nucleophiles
X
Nucleophile, solvent
R
(13)
(12) Microwave
Reactions of haloanthracene with nucleophiles
c) Coronene: Coronene (also known as superbenzene) is a polycyclic aromatic hydrocarbon (PAH)

comprising six peri-fused benzene rings. Its chemical formula is C24H12.
1. Coronene: Coronene was synthesised using microwave irradiation (850 W) for 30 min in the
microwave oven. The red brown anhydride was crystallized from the solution, recrystallized from
xylene. 4 g pure (16) was obtained (yield: 96 %). 1, 12-Benzoperylene (17): 3 g (16) (8.7 mmol) was
dissolved in 30 ml quinoline with 0.1 g copper powder. Irradiate the reaction mixture for 5 h. It
gives 1.9 g of benzoperylene (yield: 80 %). Coronene-1, 2-dicarboxylic anhydride (18): 1 g (3.7
mmol) benzoperylene was dissolved in 10 mL nitrobenzene with 0.4 g (4 mmol) maleic anhydride.
The mixture was irradiation for 1 h, 0.1 g of (18) was obtained (yield: 10 %). [12]
O
O
O
O
O
a
O
b
(14)
(15)
O
(16)
O
O
O
O
(17)
(18)
(19)
The synthetic route of coronene

II (i) a) Quinoline: Quinoline is a heterocyclic aromatic organic compound with the chemical
formula C9H7N. It is a colorless hygroscopic liquid with a strong odour.
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2, 4-dimethoxyquinolines (21): Mixed well 2, 4-Dichloroquinoline (20) (1 mmol), tetrabutyl

ammonium bromide (TBAB, 200 mg), sodium methoxide (108 mg) and few drops of water and
irradiated at 160 W under microwave condition. [13]
Cl
OCH3
NaOCH3
Cl TBAB/H2O
mw
N
(20)
R
N
(21)
OCH3
1a, 2a R = H; 1b, 2b R = 6-CH3; 1c, 2c R = 8-CH3; 1d, 2d R = 6-OCH3; 1e, 2e R = 8-OCH3

OCH3
OCH3
NaOAc/AcOH
R
N
OCH3
mw
N
H
(23)
(22)
2a, 3a R = H; 2b, 3b R = 6-CH3; 2c, 3c R = 8-CH3; 2d, 3d R = 6-OCH3; 2e, 3e R = 8-OCH3

1. 4, 6-dimethylquinoline. 4-methyl aniline (214 mg, 2 mmol) and methyl vinyl ketone (175 mg, 2.5
mmol) was mixed and the mixture was added to silica gel impregnated with indium chloride (132
mg, 0.6 mmol), prepared by adding a solution of InCl3 in minimum amount of THF to silica gel
(activated by heating for 3 h at 1500C under reduced pressure) followed by complete evaporation of
solvent under vacuum. The whole mixture was stirred for 5 min and was then irradiated by
microwave in a domestic microwave oven at 600 W (50% of total power) for 10 min (5+5 min with
an intermission of 10 min in between) to complete the reaction. [14]
R3
O
R
+ R3
NH2
R1
(24)
O
+
R
(27)
NH2
R2
InCl3/SiO2
MW
R
N
(26)
(25)
R2
InCl3/SiO2
R1
MW
N
(29) H
(28)
b) Indole: Indole is an aromatic heterocyclic organic compound. It has a bicyclic structure,

consisting of a six-membered benzene ring fused to a five-membered nitrogen-containing pyrrole
ring. Indole is a common component of fragrances and the precursor to many pharmaceuticals.
Compounds that contain an indole ring are called indoles.
1. Indole-2-carboxylates: Compound (30) in toluene was irradiated in microwave for 15 min at
2000C and a pressure of 8.1 bar to give full conversion to the corresponding indole. [15]
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COOMe
i
COOMe
N3
NH
R
R
(30)
(31)
Scheme2. Synthesis of indole-2-carboxylates, Reagents and conditions: (i) MW, n-hexane, 2000C,
10 min, 15 bar.
2.
Spiro compound 36/37: Compound (32) (2 mmol) and malononitrile (2 mmol) in absolute
ethanol (5-10 ml) in the absence/presence of piperidine (1 drop) was mixed and the mixture was
irradiated at 340/275 watts. As the reactants disappeared, (34)/ (35) was added, mixed thoroughly
and again irradiated. [16]
S
C6H5N
CN
CN
CN
CH2
CN
NH
S
O
C6H5N
(34)
N O A/B/C/D
H
(32)
N
H
O
NH2
NH
N O
H
(36)
(33)
CN
O
O
O
NH2 (35)
X
S
NH
C6H5N
(33)
(34)
N
H
CN
OH
NH
C6H5N
CH
CN
O
CN
N
H
(37)
CH
O
NH
C 6H 5N
CN
N
H
3.
CN
O
NH2
X
N
H
CN
(38)
2-(4-tert-butylphenyl)-1H-indole: 4-tert-butyl-N-o-tolylbenzamide (300 mg, 1.12mmol)
and potassium tert-butoxide (268 mg, 2.8 mmol) were mixed and it was irradiated in a microwave
oven (power 1000W) for 20 minutes, reaching a maximum temperature of 330 C. [17]
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1. THF, - 400C
2. NH4Cl aq
+ 3 MgBr
NO2
(39)
N
H
(41)
(40)
Bartoli synthesis
NH2
NH
R
(46)
N
H
(44)
O
2. MeSC(CO)R3
3. base
4. Raney - Ni
NaOEt
3600C
Madelung synthesis
1. t-BuOCl
N
R
(47)
O
(48)
Gassman synthesis
N
H
(42)
Hegedus synthesis
1. DMF/DMA
N
NO2 2.Ni/H2
H
(43)
Batcho- Leimgruber synthesis
1. Pd(II)
2. red
CO2Et
+
H2N
(45)
CO2Et
HO
N
H
(50)
(49) Nenitzescu synthesis
CH3
Br
+
N
H
NH2
(51)
(52)
(53)
Bischler- Mohlau synthesis
t- BuOK
N
H
(54)
MW, Tmax 1600 C
N
H
40%
t- BuOK
MW, Tmax 1800 C
N
H
(55)
O
N
(56)
N
H
64%
t- BuOK
MW, Tmax
R
0
160 C N
N
H
(57)
R= H, 15%, R= t-Bu, 22%
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c) Synthesis of Isoindole: Isoindole in heterocyclic chemistry is a benzo-fused pyrrole. The

compound is an isomer of indole and its reduced form is an isoindoline. Isoindoles are building
blocks for phthalocyanines which are relevant as dyes.
Porphyrins (62) a, b in DMSO: Microwave irradiation for 4 min at 2500C was given to get a
quantitative yield of porphyrins (62)a,b(Scheme 2). The annealed porphyrin (62) was obtained but in
a very low yield (25%). [18]
OMe
OMe
SOnPh
PhSCl
90%
OMe (58)
m-CPBA
Cl
59a
OMe (59)
n=0
59b
n=2
DBU
90%
OMe
SO2Ph
CNCH2CO2Et
OMe
OMe
(60)
OMe
R
N
H
iii. DDQ, 28%

KOH/
ethylene
i.2,4,6,-Me3-C6H2CHO/TFA
glycol
OMe
0
160-165 C
ii. DDQ, 30%
80%
NH
tert-BuOK/THF
(61) 85%
MeO
i. LiAlH4
ii. TFA
H
N
R
(62)
MeO
1.
OMe
OMe
OMe
2-Aryl-IH-Isoindole-l,3-Dione : A mixture of the corresponding phthalic anhydride (0.68 mmol)

and the aniline (0.68 mmol), without solvent, was added in 4 ml vial and then it was irradiated in a
domestic microwave oven at 550 W for 12-15 min. [19]
O
R
NH2
O +
(63) O
63, R = H
63, R = Me
R4
R2
R
(64)
Neat, 550w, 8.5 min
R
N
R1
X
R2
R3
X
(65) O R5
R4 (66)
66a-n(R = H, X = C, 34-97%)
67o ( R =H, X = N, 43%)
68a-m (R = Me, X=C, 63-97%)
d) Acridine: Acridine, C13H9N, is an organic compound and a nitrogen heterocycle. Acridine is also
used to describe compounds containing the C13N tricycle. Acridine is structurally related to
anthracene with one of the central CH groups is replaced by nitrogen.
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1. 10-Aryl-3,3,6,6-tetramethyl-1,2,3,4,5,6,7,8,9,10-decahydroacridine-1,8-dioxime (74):
Compound (69) (0.25 mmol), hydroxylamine hydrochloride (1.2 mmol) and sodium acetate (2
mmol) was mixed in ethanol (1 ml) and the mixture was irradiated for 3 min. [20]
O
O
+
ArNH2
Me
O
Me (69)
(70)
HCO2H
1500C, 23 h or Me
Me
MWI 12 min
Ar
71a Ar =Ph71b Ar =4-Cl-C6H471c Ar =pyrid -2-yl
NH2
HCO2H
Me
Me
Me
(71)
Me
NH2OH, HCl or
PhNHNH2
NR
O
O
O
CHO (69)
Me
Me
OH
O
NR
O
Me
Me
(72)
Me
Me Me
Me
O
(73)
Me (74)
Me
N
Ar
N NH2
N NH2
PhCHO
Me
N N = CHPh
O PhCHO/EtOH
Me
(81)
(75)
Me
Me
O
Ph
N N
H
Ph O
(76)
(80)
PhCHO Me
Me
Me
Me
N
N
Me
(77)
Me
Me
Me
O
CHPh
O
N
O
N
H
O
(83)
Me
Me
HO
CHPh
N
(79)
Me
Me
(78)
NH2
CHPh
O
Ph O
N
H
Ph
O
2
HCl
Me
Me
Me
Me
OHHO
(82)
Me
Me
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2.
Substituted 9-(1, 2, 3-Triazol-1-yl) acridines: 9-azidoacridine (0.005 mol) was mixed with
appropriate acetylene (0.015 mol) in toluene (10 cm3) and the mixture was irradiated in the
microwave at 80C (2535 W input power) till the completion of reaction. [21]
N
N
N3
1
+ RC
N
(84)
CR
N
N
R2
MWI
(85)
R2
R1
R1
+
N
(86)
(87)
Table 1: Microwave-Assisted Preparation of Substituted 9-(1, 2, 3-Triazol-1-yl) acridines

e) Azepine: Azepines are unsaturated heterocycles of seven atoms, with a nitrogen replacing a
carbon at one position.
1. 3-(naphtho[2,1-b]furan-2-ylcarbonyl)-3H-1, 3,4-benzotriazepine (93). A dilute solution of
compound (92) (1.6 g, 5 mmol) in triethyl ortho formate was irradiated until completion of the
reaction. [22]
CHO
OH CICH COOC H
2
2 5
DMF / K2CO3
MW / 3-4 min
(88)
O
(89) O
OC2H5
Ethanol /H+
NH2NH2H2O
MW / 4-5 min
R3
OHC
R2
(93)
H2N
R3
R2
N
N
N
R
NH2
(90)
Ethanol / H +
MW / 2-3 min
(91)
O
NH2
R1
R
O
R1 MW / 2-3 min
Triethyl ortho formate
R3
NH
(92)
R2
R1
H2N
R
General synthetic procedure of naphtho[2,1-b]furan-1,3,4-benzotriazepines (93)

f) Pyrrole: Pyrrole is a heterocyclic aromatic organic compound, a five-membered ring with the
formula C4H4NH.
1. Pyrroles (98): A 5 ml microwave reactor vial, equipped with a magnetic stirring bar and fitted
with a rubber septum, was charged with azide (97) (1.00 mmol) and 1,2-dichloroethane (2 ml). Zinc
chloride (1.0 M in ether) was added dropwise with a syringe and then capped the vial. The reaction
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0
was carried out at temperature 105 C, run time 60 min, power high (pressure ca.2 bar). [23]
R
R'
O
+H
OH
N3
i-Pr2NLi
1. MsCl,Et3N
R
R
CH2Cl2
R DMSO
R'
R'
or n-BuLi
'
'
2. NaN3, DMF
R
R
(97)
BF3 - Et2O
(96)
or(PhO)2P(O)N3
THF
(CH2Cl)2
DIAD,Ph3P,THF
ZnCl2
MW or
H
R N R''
''
(95)
(94)
R'
Synthesis of pyroles .
2.
(98)
1, 4-diketo-pyrrolo [3, 4-c]-pyrroles (101). Mix benzonitrile (0.21 g, 2 mmol), ethyl
bromoacetate (0.50 g, 3 mmol) and Zn-Cu couple (0.4 g) and place it in a 25-ml beaker and was
inserted into a screw-capped Teflon beaker and irradiated in a microwave oven at high power for 10
min to get the pure product (101) (0.41 g, 71%). [24]
Ar
Ar
O Zn - Cu
CN +
MW/ solvent - free HN
(99) BrH2C
OEt
O
(100)
O
NH
Ar
(101)
g) Carbazole: Carbazole is an aromatic heterocyclic organic compound. It has a tricyclic structure,

consisting of two six-membered benzene rings fused on either side of a five-membered nitrogencontaining ring. The compound's structure is based on the indole structure but in which a second
benzene ring is fused onto the five-membered ring at the 23 position of indole.
1. 3-bromocarbazole-N-acetic acid: 3-bromocarbazole (4.9 g, 0.02 mol), sodium hydroxide (5.7 g,
0.1 mol), and the ethyl bromo-acetate (4.3 g, 0.026 mol) was mixed in DMF was heated in a
domestic microwave oven in an open round-bottomed flask for 4 min. [25]
Br2
N
H
(102)
00C
Br
Br
BrCH2COOC2H5
N
N
KOH/DMF
H (103)
Microwave
(104) CH2COOH
- 189 - | P a g e
2. 6,7,8,9-tetrahydro-1-methoxy-3-nitro-5H-carbazole: The intermediate 6,7,8,9-tetrahydro-1methoxy-3-nitro-5H-carbazole (106) was obtained by an indole-modified Fischer synthesis from 2methoxy-4-nitro-hydrazine (105) by microwave-assisted one-pot synthesis, in order to shorten the
synthetic pathway to our final compounds (Scheme 1A and B). The synthesis of tetra hydro pyrido
carbazoles was done by condensing 2-ethoxy-4-nitro-phenyl hydrazine
chloride (105) with
cyclohexanone and this was submitted to acid cyclization to carbazole (106).The optimization of the
method was done with the aim of increasing the yield: first, the power set point was 100 W and the
temperature reached was 1000C. The conditions were then maintained constant by a cooling system
for 6 min yielding 67% (experiment 1). [26]
A
O2N
c) cyclohexanone,
O2N
acetic acid
N
H
MW
NHNH2
OCH3
(105) OCH
3
(107)
a) cyclohexanone
O2N
b) H2SO4 4%
R
B
NHNH2
MW
c) cyclohexanone,
acetic acid
N
(109)
R
(108)
b) CH3COOH, H2SO4
a) cyclohexanone
NH N
OCH3
(106)
N
H
NHN
N
(110)
R
3. N-arylation of carbazoles: Add 9H-Carbazole (1.0 mmol), Cs2CO3 (1.0 mmol), iodobenzene
(1.1 mmol), CuI (0.1 mmol), and DMF (2 ml) to a 5-mL vial. Sealed the vial with a crimp cap and
placed the vial in a microwave cavity. Irradiate vial at 220 0C. N-Phenyl-carbazole (114) was
obtained (96% yield) as a white solid. [27]
Br
+
N
H
10 mol% Cu
1 eq Base,2200c
Microwave, 1h
(111)
N
(112) Ph
Optimization of conditions for Cu-catalysed N-arylation of carbazoles
N
H
(113)
10% CuI, 1eq Cs2CO3

+ X-Ar
R2
MW, DMF, 2200C R
N-Arylation of carbazoles with arylhalides
N
Ar
(114)
R2
- 190 - | P a g e
h) Quinoxaline derivatives: A quinoxaline, also called a benzopyrazine, in organic chemistry, is a

heterocyclic compound containing a ring complex made up of a benzene ring and a pyrazine ring. It
is isomeric with other naphthyridines including quinazoline, phthalazine and cinnoline.
1. 3, 5-Disubstituted pyrazolyl Derivatives (119): Prepare solution of compound (117) (1.0 g, 5.7
mmol) in -diketone (5.7 mmol), and add ethanol (10 ml). Then the mixture was irradiated in a
domestic microwave oven at an emitted power of 400 W for the appropriate period. The clear
solution formed was left to stand at room temperature to crystallize. Crude solid product was
recrystallized from the appropriate solvent to afford 3, 5-disubstituted (pyrazol-1-yl) quinoxalin2(1H)-one. [28]
NH2
NH2
(115)
H
N
OH
OH
H
N
N
H
H
N
ii
N NHNH2
(117)
(116)
keto - enol tautomerism
O
iv
O
N
(118)
H
N
iii
N
N
N
(120)
(119)
R1
N
N
R
(ii) a) Pyrazole: Pyrazole is the organic compound with the formula C3H3N2H. It is a heterocycle
characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen centres.
Pyrazoles are also the class of compounds that have the ring C3N2 with adjacent nitrogen centres.
1. 3, 5-Disubstituted pyrazolyl Derivatives (127): Add ethanol (10 ml) to a solution of compound
(124) (1.0 g, 5.7 mmol) in -diketone (5.7 mmol), and the reaction mixture was irradiated in a
domestic microwave oven at an emitted power of 400 W till the completion of reaction. [29]
NH2
NH2
(121)
OH
H
N
OH
N
H
(122)
H
N
ii
O
(123)
N NHNH2
(124)
keto- enol tautomerism

H
N
N
(126)
N
N
iv
(125)
iii
H
N
R1
N
(127)
N
N
R
- 191 - | P a g e
2.
3-substituted phenyl-5-substituted phenyl-4, 5-dihydro-pyrazole-1-carbothioamides (131):

Mix chalcone (128) (0.022 mol) and thiosemicarbazide (0.02 mol) and dissolved the mixture in
acetone (5 ml) and ethanol (5 ml), respectively. Add basic alumina (4 g) and stirred vigorously.
After 5 min, remove the solvent under vacuum and the dry powder was irradiated in a microwave
oven, at 650 W. [30]
O
R1
CO - CH3 + H - C
R2
(128)
C2H5OH
Microwave NaOH
-H2O
C
R2
Microwave
CH
(129)
CH
(130)
Microwave
OC - NH - NH2
S
H2N C NH - NH2
Basic alumina / K2CO3
R1
R1
N
R2
O
(131)
N
C
R1
R2
N
C
H2N S
N (132)
Synthesis of title compounds (131) and (132)

b) Indazole: Indazole, also called benzpyrazole or isoindazone, is a heterocyclic aromatic organic
compound.Indazole derivatives display a broad variety of biological activities. Indazoles are rare in
Nature.
1. 6-(2-hydroxyphenyl) -4-aryl 3-oxo-2, 3, 4, 5 tetrahydro-1H indazoles: Mix thoroughly 6Carbethoxy cyclohexenones (0.01 mole) and hydrazine hydrate (0.015 mole) to form intimate
mixture. Then subject it to microwave irradiation for 4-8 minutes. Completion of the reaction was
indicated by TLC. Colourless crystals of indazoles separated out which were filtered. [31]
OH
OH
OH
Ar
b
AH H Ar
AH HB Ar
a
B
Hc
Hc
O
C - O - CH2 - CH3
O
(133)
(134)
O
N NH
O
(135)
a. CH3COCH2COOC2H5 \ Anhy. K2CO3 or CH3COCH2COOC2H5 /Basic Alumina, MWI, 5-7 min. b
NH2NH2. H2O, MWI, 4-8 min
- 192 - | P a g e
2. 2-{(2E)-2-[1-(2- chlorophenyl) ethylidene] hydrazino}-3 substituted phenyl -1, 8naphthyridine (138) :Mix 3-aryl-2-hydrazino-1, 8- naphthyridines (136) (0.01 mol), substituted
acetophenones (137) (0.01 mol) and methanol (30 ml) with a few drops of glacial acetic acid and
then exposed to microwave irradiation at 150 watts for 2 min to give product (139). [32]
Cl
Ar
Cl
O
Ar
Ar
N
C
N N N
+ H3C
DMF/KOH
C
Methanol/ N N NH
N
N N NHNH2
MW
(137) CH3COOH
(138)
(139)
CH3
CH3
(136)
c) Imidazole: Imidazole is an organic compound with the formula (CH)2N(NH)CH. It is a colourless
solid that dissolves in water to give mildly alkaline solution. In chemistry, it is an aromatic
heterocycle, classified as a diazole and as an alkaloid.
1.
2 amino 1H 4 phenylimidazole (141): A mixture of 2 phenylimidazo[1,2 a]pyrimidine (140) and

20% hydrazine hydrate in a suitable solvent was irradiated in a sealed vial at 150W maximum
power. [33]
N
N
20% N2H4/ETOH
N
MW,120 0C
N
H2N
R1
N
H
(141)
R1
(140)
Microwave-assisted synthesis of 4(5)-substituted 2-amino-1H-imidazoles 175a-ka
2.
5-Substituted-2-(2-methyl-4-nitro-1-imidazomethyl)-1, 3, 4-oxadiazoles (144): Mix substituted

carboxylic acid (001 mol) and hydrazide (142) (001 mol) and the mixture was ground in a mortar
using a pestle for uniform mixing. Take this mixture in a 50 mL beaker and 56 drops of
phosphorous oxychloride was added. Keep the beaker a microwave oven at 160 W for about 5 min.
to give crude product (144). [34]
O2N
3.
CH2CONHNH2
N
+ RCO2H
N CH3
(143)
(142)
POCl3, MW
N
O2N
POCl3,
R
N
N CH3
(144)
Trisubstituted imidazoles: Place benzil (0.5 mmol), p-methylbenzaldehyde (0.5 mmol):
ammonium acetate (4 mmol) and glacial acetic acid (0.6 g) in a tube and mixed thoroughly. The
mixture was irradiated in the microwave oven with 638W for 5 minutes. [35]
- 193 - | P a g e

Ph
Ph
Ph
O
HOAc
N
+ ArCHO + NH4OAc
Ar
MW Ph
(146)
N
(147)
O
H
(145)
(148)
d) Quinazoline: Quinazoline is a heterocyclic compound made up of two fused six-membered

simple aromatic rings, a benzene ring and a pyrimidine ring. Its chemical formula is C8H6N2. It is
isomeric with other naphthyridines including quinoxaline, phthalazine and cinnoline. Derivatives of
quinazoline are called quinazolines.
1. Bis-quinazolines (152) & (153). Diamine (0.5 mmol) and formaldehyde (2 mmol, 40% aqueous
solution) in 1.5 ml methanol was mixed and then mixture was shaken at room temperature for 5 min.
A solution of enaminone (150) (1 mmol) in 5 ml methanol was added to the mixture in one lot and
the resulting mixture was irradiated in a microwave for 24 min at 180 W at 60C, yielding (152)
and (153) in 5179% yields. [36]
O
(149)
O
PhCH2CH2NH2
O
R1NH2/CH2O
R
R
O
O
N
R R
NH2-(CH2)n-NH2
[]n N
N1
N1
R
R
R
R
CH2O/MeOH/MWI
(152)
O
R
R
N
(151)
(150)
R
H2N
NH2
2a H
2b Me
CH2O/MeOH/MWI
O
N
R R
NH
MeOH/MWI
N1
N
n N'
1
(153)
2. 2, 7-dicyano-9-ethoxythiazoloquinazoline: Starting amine was condensed with 4, 5-dichloro-1,

2, 3-dithiazolium chloride (154) in dichloromethane, in the presence of pyridine, to give the imino-1,
2, 3-dithiazole (160). This imine was irradiated with sodium hydride in ethanol at 300 W for 10 min
to give 4-ethoxy-6-nitroquinazoline-2-carbonitrile (161). Condensation of amine (163) with the salt
- 194 - | P a g e
(154) gives dithiazole (164). It was converted exclusively into the angular 2, 7-dicyano-9ethoxythiazoloquinazoline (165) with cuprous iodide. [37]
Cl
NH2
R
X
(154)
S+
Cl- S
Cl
(45)
S
Cl
CuI,pyridine
CN
X=Br
S S
X
(155)
pyridine, r.t.
ROH
N
Nah
CN
N
OR
X=CN
NC
H2N
S SNC
NO2
N
a
N
Cl
(159)
(158)
NH2 e
N
NC
NO2
b
NC
OEt Br
OEt Br
NC
(162)
NO2
N
N
(160)
S S
(163)
NH2
d
N
NC
N
(161)
O
CN
Cl
N
(157)
OEt
OEt
(156)
OEt S
f
N
NC
N
(164)
S
N
g HN
N
(165)
Reagents and conditions (for time and yields of steps b, c, f and g: see Table 1): (a) 1, pyridine, rt,
10 h, 78%; (b) NaH, EtOH, reflux; (c) SnCl2.2H2O, EtOH, 70C; (d) Br2, CH3COOH, rt, 4 h, 74%;
(e) 1, pyridine, rt, 4 h, 66%; (f) CuCN,pyridine, reflux; (g) HCl, reflux
e) Benzimidazole: Benzimidazole is a heterocyclic aromatic organic compound. This bicyclic
compound consists of the fusion of benzene and imidazole.
1. Benzimidazole: Mix o-phenylene diamine (166) and formic acid (167) and place the mixture in a
microwave oven. [38]
NH2
NH2
+
(166)
2.
OH O 10% NaOH
(167)
H
N
N
(168)
2-(alkyloxyaryl)-1H-benzimidazole: Benzimidazole have been synthesized by treating 1, 2-
phenylenediamine with adequate aromatic substituted aldehydes, utilizing sodium metabisulfite

- 195 - | P a g e
under microwave irradiation (Scheme 1). The reactions were performed without solvent in only 60 s
as a maximum time. [39]
NH2 O
+
NH2 H
(169)
Ar + Na2S2O5
Ar
irradiation
(30-60 sec)
(171)
(170)
Microwave
N
H
(172)
(75-94%)
Preparation of 2-(alkyloxyaryl)-1H-benzimidazolederivatives
Compound (175) was obtained with low yield from (Scheme 1), using an excess of alkylating agent
iodoethane (Scheme 2). When microwave irradiation time was extended, it was possible to observe a
decrease of the yield due to formation of several by products.
N
N
H HO
+ CH3CH2I(Excess)
K2CO3
Acetone
(174)
(173)
(175)
Synthesis of 2-(2-ethoxyphenyl)-1 ethyl-1H-benzimidazole (177)
3. 1, 3-diarylpyrazino [1, 2-a] benzimidazoles (181): Compound (180) (1 mmol) and ammonium
acetate (10 mmol) was mixed in 0.5 ml of acetic acid. Irradiate the mixture at power 600W in
microwave oven for 2 min. [40]
R
N
N
H
R
i, ii
Cl
N
H
(177)
(176)
+
(178)
O
R
O
Br
R'
(179)
iii
N
N
iv
O
O
N
N
N
(181)
(180)
R'
R'
Reagents and conditions; (i)(C2H5)3N, pyridine, stirring at RT; (ii) NaOH, H2O, reflux;
(iii) K2CO3, CH3COCH3, stirring at RT; (iv) CH3COONH4, CH3COOH, MW irradiation,2 min.
4. Pyrimido[1,2-a]benzimidazoles : Mix thoroughly the 2-aminobenzimidazole (182) (1 mmol) with

the acetophenone derivative (183) (2.1 mmol) in the presence of catalytic amount of acetic acid (one
- 196 - | P a g e
drop~0.2 mmol). At the temperature of 1600C only the Schiff bases (184) were isolated, with
exception of the 1-naphthyl derivative, which was formed at 2500C. Increasing the temperature to
250 0C led to the synthesis of only derivatives (185), with exception of the bromosubstituted ones,
which were formed at 200 0C to afford compounds (184) or (185). [41]
R2
N
N
H
(182)
NH2
R1
COMe
R1
N
N
H
(183)
R2
Me
(184)
N
N
R1
R2
R1
Me O
(185)
R2
Reagents and conditions: (a) MW irradiation, 160 C, 4e10 min; (b) MW irradiation, 2500C, 5-10
min including catalytic amount of acetic acid in both cases (molar ratio of
benzimidazole:ketone:acetic acid 1:2.1:0.2).
0
5. 2-(2-ethoxyphenyl)-1ethyl-1H-benzimidazole(192):The reaction of 1,2-phenylene diamine with

adequate aromatic substituted aldehydes, utilizing sodium metabisulfite under microwave irradiation
(Scheme 2) gives the derivatives of benzimidazole. All reactions were performed without solvent in
only 60 s as a maximum time, confirming that the focused microwave irradiation. [42]
NH2
O
+
NH2
(186)
Microwave
Ar + Na2S2O5
irradiation
(187) (188) (30-60 sec)
N
Ar
N
H
(189)
(75-94%)
Preparation of 2-(alkyloxyaryl)-1H-benzimidazolederivatives
N
N
N
H HO
+ CH3CH2I(Excess)
(191)
K2CO3
Acetone
N
O
(192)
(190)
Synthesis of 2-(2-ethoxyphenyl)-1 ethyl-1H-benzimidazole (192)
(iii) a) Purine: A purine is a heterocyclic aromatic organic compound. It consists of a pyrimidine

ring fused to an imidazole ring. Purines, including substituted purines and their tautomers, are the
most widely occurring nitrogen-containing heterocycle in nature. Purines and pyrimidines make up
the two groups of nitrogenous bases, including the two groups of nucleotide bases.
- 197 - | P a g e
1. 3-Butyl-11-cyclopentyl-6,7,8,9-tetrahydrodiazepino[1,2,3-cd]purine-2,4-dione (196): Add to a

solution
of 8-butyl-10-cyclopentane carboxamido-1,2,3,4,5,7,8,9-octahydro pyrimido [1,6-]
[1,3]diazepine-7,9-dione (194) (0.17 g, 0.5 mmol) in THF (1 ml) in a 10 ml pressure vial, HMDS (1
ml). Microwave irradiation was applied (200 W, 160C) for 20 min. The resulting yellow solution
was hydrolyzed with 4 ml of methanol while still warm (ca. 50C). Compound (196) (0.15 g, 91%)
was obtained as a yellow oil. [43]
O
H3 C
O
H
N
O
O N NH
(193)
( )n
193(n = 0)
194(n = 1)
195(n = 2)
H 3C
HMDS / THF
N
O
(194)
( )n
196(n = 1)
197(n =2)
Microwave-supported synthesis of pyrimido- and diazepino-purinediones
b) Pteridine: Pteridine is a chemical compound composed of fused pyrimidine and pyrazine rings.
A pteridine is also a group of heterocyclic compounds containing a wide variety of substitutions on
this structure. Pterins and flavins are classes of substituted pteridines that have important biological
activity.
1. Pterin sugars: Synthesis was done by a simple direct condensation without addition of sodium
bisulphite or hydrazine hydrate under microwave irradiation. A mixture of triamine (198) and
methylglyoxal was irradiated in an open flask using a household microwave oven to obtain 70%
yield. Condensation with 1, 3-dihydroxyacetone (DHA) and 1, 1-dichloroacetone also led to the
formation of (199) a only, but in a poor yield. However, this condensation reaction further prompted
us to irradiate the triamine (198) and aldohexoses, which gave the pterin sugar derivatives (199) c
and (199) e with the expected side-chain length and functionality at each of the four carbon atoms.
[44]
O
HN
H2N
NH2
HN
carbonyl compound
MW
RHN N
N NH2
(198)
R'
N
(199)
- 198 - | P a g e
III) (i) a) Benzofuran: Benzofuran is the heterocyclic compound consisting of fused benzene and
furan rings. This colourless liquid is a component of coal tar. Benzofuran is the "parent" of many
related compounds with more complex structures.
1. Benzo[b]-furan derivatives: Thoroughly mix potassium carbonate (2.70 g, 20 mmol), TBAB
(0.16 g, 0.50 mmol), and a salicylaldehyde derivative (5.0 mmol) and placed the mixture in an open
conical glass flask. Then add dropwise a chloroacetate ester (10 mmol), the mixture was thoroughly
stirred with a spatula for a few seconds, place mixture in a domestic microwave oven, and irradiated
for 810 min. [45]
CHO
R1
R
+ Cl-CH2-CO2 -R3
K2CO3/TBAB
OH
mw, 8-10 min
(201)
(200)
R3:Et
R3:CH2CH=CH2
OH
CHO + Cl-CH -CO -R3 K2CO3/TBAB
2
2
mw,8-10 min
(203)
(204)
R1
R
CO2-R3
(202)
R3:cyclohexayl
O
CO2-R3
(205)
(b) Chromene: Benzopyran is an polycyclic organic compound that results from the fusion of a
benzene ring to a heterocyclic pyran ring. According to IUPAC nomenclature it is called chromene.
There are two isomers of benzopyran that vary by the orientation of the fusion of the two rings
compared to the oxygen, resulting in 1-benzopyran (chromene) and 2-benzopyran (isochromene)
the number denotes where the oxygen atom is located by standard naphthalene-like nomenclature.
1.
4-oxo-2-phenyl-4H-chromen-3-yl 4-methoxy benzoate (210):3-hydroxyflavone (0.95 gm, 0.004

mol) and p-methoxybenzoyl chloride (1.023 gm, 0.006 mol) was mixed and was irradiated in a
microwave oven for 3 minutes. The completion of reaction was monitored by TLC and FeCl3. [46]
- 199 - | P a g e

EtOH
40%NaOH
R
1
H
Cl CH R -CHO
OH i)ArCl
CH3COONa
ii)AlCl3
R
(206)
OH
OH
R
(207)
O
(208) O
NaOH
30% H2O2
EtOH
R1
R
(210)
2.
O
O
C R2
O
R -COCl
CM MWM R
R1
OH
(209)
3-nitro-2H-chromene derivatives: Thoroughly mix dry potassium carbonate (2.70g,
20mmol), tetrabutylammonium bromide TBAB (0.16g, 0.5mmol) and a salicylaldehyde derivative

(4.0mmol) and placed it in a small transparent polypropylene beaker. Irradiated the reaction mixture
for 2 min using 20 % of the maximum power of oven. [47]
R
O
C
NO2
H+
K2CO3 / TBAB
HO -CH2CH2 -NO2
O H
R
MW 140 w 2 min
(211)
(210)
3.
4H-chromene derivatives (242): Thoroughly mixphenoxypyrazole-4-carbaldehyde (235)
(10 mmol), malononitrile (236) (10 mmol) and Cyclohexanedione/Dimedon (237) (10 mmol) in
ethanolic NaOH (5 mmol, 10 mL) and irradiated in microwave oven at 350 W (50% of output
power) for 140-170 sec, to get the pure solid product (238). [48]
- 200 - | P a g e
H3C
CHO
H3C
N
DMF
Cl
CHO
H3C
N
R1
(213)
(212)
R1
(215)
OH
K2CO3
R2
R2
R1
(214)
CHO
(219)
(215)
O
H3C N N
+
NaOH, Ethanol
+
O
O
NC R3
MWI 350W,
CN
R1
O 140-170S 3
R
R2 (216)
(217)
R3
O NH2
CN
CN -H2O
(216)
R1
R2
NC
(218)
O
Pyz +
DMF
POCl3
CHO
H3C
Pyz
NC
NC
R3
3
R
HO
CN
(220)
Hetarylidene
-nitrile
Pyz O
NC
H2N
Pyz
R3
R3
HO
R3
R3
(221)
Pyz O
NC
HN
O
H
R3
R3
(222)
c) Xanthene: Xanthene (9H-xanthene, 10H-9-oxaanthracene) is a yellow organic heterocyclic
compound. Its chemical formula is C13H10O.
1. 1, 3-Dialkylxanthines (1 and 2): 1 g of 5,6-diamino-1,3-dialkyluracil (5 mmol of 3 or 4 mmol of
4, respectively) and triethyl orthoformate (6 ml) was mixed and it was subjected to microwave
irradiation for 5 min (120 W, 160C) in a 10 ml pressure tube, with stirring. [49]
- 201 - | P a g e

R1
N
O
O
NH2
N NH2
R3 (223)
H
N
N
R3
N
(224)
HC(OEt)
MW
5 min/ 1600 C
Microwave-assisted preparation of xanthine derivatives

(ii) a) Coumarin: Coumarin (2H-chromen-2-one) is a fragrant organic chemical compound in the
benzopyrone chemical class.
1.
Tetrakis-(4-hydroxy-2H-1-benzopyran-2-ones) (227): One of dialdehydes (225) was
mixed with (226) (1.0 mmol) and 4-hydroxy coumarin (4.0 mmol) in 4 mL of DMF and 5 drops of
acetic acid was added. The mixture was heated in a microwave for about 5 min. [50]
O
O(OCH2)
(225) OH
DMF
+
Microwave
O(CH2)nO
CHO
(226)
O
O
O
OH OH
CHO
O
OH OH
(227)
Synthesis of tetrakis-(4-hydroxy-2H-1-benzopyran-2-ones)
2. 3-Acetylcoumarin (230): Catalytic amount of piperidine (0.2ml, 1.64 mmoles) was added to a
mixture of salicyaldehyde (0.86 ml, 81.89 mmoles) and ethyl acetoacetate (11.5mL, 90.13 mmoles)
and swirled thoroughly. The mixture was then irradiated in microwave oven at 400 W for 1 min.
Filter the solid product, dried, and recrystallized from methanol to obtain pure 3-acetyl coumarin
(230) in appropriate yield. [51]
O
CHO
CH3
Piperidine
+ CH3COCH2CO2C2H5
MWI
O O
OH
(230)
(229)
(228)
Microwave assisted synthesis of 3-acetylcoumarin
- 202 - | P a g e
3. 3-aryl- furo[3,2-c]coumarins(266): Method A: Stir a solution of appropriate 4-hydroxy coumarin

(264) (0.002 mol) and 2-aryl-1-nitro-ethenes (265) (0.002 mol) in methanol (5 ml) containing
piperidine in catalytic amount at room temperature for 10 min. Then irradiate it for 57min in
microwave at 240W (40%) power, to afford the compounds (266).
Method B: Add a solution of appropriate 4-hydroxy coumarin (264) (0.002 mol) and aroylmethyl
bromide (265) (0.002 mol) in acetic acid (4 ml) ammonium acetate (0.01 mol) at room temperature.
Stirred the reaction mixture at room temperature for 10 min and then irradiated for 23 min in
microwave
at
240
(40%)
power,
to
afford
the
compounds
R1
(266).
[52]
R1
O
R
7
OH
(231)
5
O
R1
6
(a)
R
4O
R 8 9
O 2
1
R2
4'
'
OH
(231)
+
(b)
R2
R2
(234)
Br
O
(232)
O2N
(233)
Synthetic scheme for 3-aryl-furo[3,2-c]coumarins 4a-I. (a)Piperidine,Methanol, mw (b) NH4OAc, AcOH, mw
4. Coumarins: Condensation of phenols (267) with -keto esters (268) gives the coumarins
(Scheme 1). A mixture was irradiated with microwaves of low power (200 W). The temperature of
the reaction mixture started to rise. After 30 s of irradiation, the microwave oven was switched off.
[53]
R
+
R
OH O
(235)
CHO
+
OH
(239)
CH2CO2Et
(240)
R'
(236)
CH2(CO2Et)2
R'
(237)
(238)
CO2Et
O O
(241)
5. 3-(20-amino-30-cyano-40-arylpyrid-60-yl) coumarins: Aromatic aldehyde (1 mmol), 3-acetyl

coumarin (1 mmol), malononitrile (1 mmol), ammonium acetate (2 mmol) and acetic acid (5 ml)
was mixed into an erlenmeyer flask (25 ml) equipped with reflux condenser. Irradiate the reaction
mixture in a microwave oven for 1013 min (as indicated by TLC). [54]
- 203 - | P a g e

Ar
O
CN
CH3
+ ArCH2O + CH2(CN)2
O
(244)
(243)
NH2
O O
(245)
(242)
IV) a) Benzothiophene: Benzothiophene is an aromatic organic compound with a molecular

formula C8H6S and an odour similar to naphthalene (mothballs). It occurs naturally as a constituent
of petroleum-related deposits such as lignite tar. Benzothiophene has no household use. It is used
primarily in industry and research.
1. 1,5-benzothiazepines: Substituted 2-hydroxychalcones (246) (0.01 mol), o-aminophenol (247)
(0.012 mol) and piperidine (3-4 drops) in 2-methoxyethanol (10 ml) was added in a round-bottomed
flask, then it was irradiated in microwave oven for 4-6 minutes (TLC), with short interval of time
for 10 sec, to give corresponding 1,5-benzothiazepines (248). [55]
Ar'
ArCOCH=CHAr'
SH
+
H2N
(246)
2 -methoxyethanol
(247)
Piperidine, MWI
4-6 min
N
(248)
Ar
Synthesis of 1, 5-benzothiazepines.
2. 2-arylbenzo[b]thiophenes: The cyclization with the symmetrical substrate 1g having two ortho
methoxy groups on aromatic rings was performed at 1300C within 1 h in the microwave, the reaction
took place smoothly to provide the desired compound (250) together with starting material 1g. By
increasing the temperature to 1600C, the reaction went to completion and (250). [56]
R1
XR
(249)
PTSA (1.0 eq)

Microwaves
R1
X
(250)
X = O,S
Reaction of ortho-substituted arylalkynes 1 with PTSA in EtOH: synthesis of 2-arylbenzo[b]furans
and 2-arylbenzo[b]thiophenes
3.
Benzo[b]thiophenes: Benzaldehydes (251) were reacted with rhodanine and after hydrolysis with
sodium hydroxide to obtains, the corresponding b-aryl-amercaptoacrylic acids (252) in good yeilds.
The acids (252) can then be cyclised and decarboxylated to give the corresponding
benzo[b]thiophenes (253). The reaction was carried out directly on a 170mmol scale in a 1L round
bottomed flask in a microwave oven at 2000C.
- 204 - | P a g e
COOH
H
i),ii)
SH
iii), iv)
s
(253)
(252)
(251)
(i) Rhodanine, AcOH; (ii) NaOH; (iii) cyclisation; (iv) decarboxylation

o-Fluorobenzaldehydel requires a decarboxylation. (Scheme 2) [57]
R
i)
R
COOH
H ii), iii)
F
(255)
(254)
(256)
Scheme 2. Reagents and conditions; (i)LDA,DMF, -78OC;

(ii)NEt3,HCH2COOCH3, DMSO; (iii) LiOH,THF,H2O
V) a ) Benzoxazole: Benzoxazole is an aromatic organic compound with a molecular formula

C7H5NO, a benzene-fused oxazole ring structure.
1. Benzoxazoles : Mix 1.8 mmol of 2-aminophenol, 2.0 mmol of acyl chloride in 2.5 ml of 1,4dioxane (or xylene) and the mixture was treated with microwave in a sealed reaction vessel for 15
min at 210C (or 250C). Cool the reaction mixture and then transferred slowly the mixture to a
stirred solution of 1N NaOH (50 mL). The product was precipitated, filtered, washed with water and
dried in vacuo. Method A: 2.5 mL dioxane, 1.8 mM of 2-aminophenol, 2.0 mM of acid chloride for
15 min at 210C. Method B: 2.5 mL xylene, 2.7 mM of 2-aminophenol, 3.0 mM of acid chloride for
10 min at 250C. [58]
O
O
NH2
a)
NH
+ Cl
OH
(257)
base
(258)
b)
OMe
(257)
microwave
OMe
OMe
(261)
Lewis Acid
(260)
O
O Ph
(259)
O
NH2 Cl
+
OH
Ph
OMe
N
OMe
O
(262)
OMe
Scheme 1: (a) Conventional synthesis of benzoxazoles through diacylated intermediate. (b)

Microwave-assisted synthesis of benzoxazoles in a one-pot acylation/cyclization step.
- 205 - | P a g e
VI) a) Benzothiazole: Benzothiazole is an aromatic heterocyclic compound with the chemical

formula C7H5NS .
Benzothiazoles (267): Add 2- aminothiophenol (1.1 mmol), aldehyde (1.0 mmol) and PIFA (1.05
mmol) in ethanol (3 ml) to a pyrex reaction vessel. The reaction vessel was then placed in the Emrys
Optimizer and exposed to microwave irradiation (800C) for 15 min.[59]
ZH
R
PCC / Silica
Z
R
Ar
N
(264)
Ar CH2Cl2 , rt
N
(263)
Z = S,O
Z
PIFA ( 1.05 eqiv), EtOH R
ZH
Ar
N (267)
ArCHO
0
+
R
( 1.0 equiv ) MW, 80 C, 15 min
NH2
(266)
( 1.1 eqiv )
(265)
Biological activities
Half of the therapeutic agents consist of heterocyclic compounds. A large number of efforts were
made to collect the matter for different biological activities exhibited by the heterocyclic
compounds. The practice of medicinal chemistry is devoted to the discovery and development of
new agents for treating disease. Therefore, an important aspect of medicinal chemistry has been to
establish a relationship between chemical structure and pharmacological activity. Several
benz fused heterocyclic systems as indole, benzothiazole, benzimidazole, benzoxazole and many
more, have been studied and found to possess interesting pharmacological activities viz naphthalene
(anti microbial
[60]
microbial agent
, cytotoxic against cancer cell lines
[63]
, cytotoxic activity
[64]
[61]
) , anti- inflammatory
), quinoline ( anticancer
[65]
[62]
, antimycobacterial[66],
antimicrobial[67], anticonvulsant[68], antiinflamatory[69] and cardiovascular activities

activity
[71]
), indole (anticonvulsant, tranquilizer, antimicrobial activity
PPARgamma modulators
[73]
, acridine (potent MDR-reversing agents
[74]
[72]
anthracene (anti
[70]
, anti oxidant
, potent and selective
, antitumor agent
[75]
, anti
cancer activities [76], azepine (anti-cancer [77], antiviral[78], anticonvulsant[79], antidepressant[80], antiinsecticidal[81], vasopressin (AVP) antagonist [82], pyrrole (antimicrobial [83], carbazole (antibacterial,
anti-tumor
[84]
, quinoxaline (antimicrobial
inflammatory, antioxidant
[88]
, anti HIV
(HMG-CoA reductase inhibitors)
[91]
[85]
[89]
, antidepressant
[86]
, anti cancer
, pyrazole (anti microbial, antifungal
, antibacterial (antifungal)
[92]
[87]
[90]
, anti-
, indazole
, imidazole (anti fungal[93], anti-
bacterial[94], anti-inflammatory[95], analgesic[96], antitubercular[97] , antidepressant[98] , anticancer[99],

antiviral activity[100], antileishmanial
[101]
, cardiotonic[102], muscle relaxant[103], anti convulsant[104],

- 206 - | P a g e
gastrointestinal motility promoter, anti-arrhythmic

[107]
, anti tumour
[108]
, anti psychotic
[109]
[105]
, quinazoline (anti bacterial
, anti diabetic
[110]
, anti malarial
[111]
[106]
, anti fungal
, anti oxidant
[112]
anti obesity [113], benzimidazole (anti microbial [114] , cytotoxic, diuretic [115], purine (anti cancer [116]
, anti fungal [117], pteridine (anti leishmainial [118], benzofuran (anti microbial, anti inflammatory [119],
analgesic[120], anti depressant[121], anti convulsant[122], anti tumour[123], anti diabetic[124], anti HIV[125],
anti oxidant
[126]
anti microbial
, chromene (anti bacterial
[130]
and anthelmintic
[127]
, anti leishmanial
, anti inflammatory, anti bacterial

[132]
antihyperglycemic[136],
, anti inflammatory
analgesic[137],
anti
[133]
[131]
[128],
coumarins (anti tumour
[129]
, benzothiophenes (antimicrobial, analgesic
benzoxazole (anti microbial
cancer[138]
antitubercular
[139]
[134]
, CNS[135],
benzothiazole
(antitumor[140], antimicrobial[141], anthelmintic[142] , anticonvulsant[143], anti-inflammatory[144],

antioxidant [145] , antidiabetic [146]. Therefore it has been concluded that fused heteroyclic compounds
are said to be backbone of our medicinal industry.
Conclusion
In conclusion, it has been proved that fused heterocyclic compounds are versatile organic
compounds as they can not only be synthesized by various methods but also potent biologically.
Moreover, microwave assisted synthesis worked much upon the problems like poor yield, lower
reaction rates, environment hazardous chemical reaction, use of toxic solvents by conventional
methods. There are much future prospects in this direction yet to be explored.
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International Standard Serial Number (ISSN): 2319-8141

INTERNATIONAL JOURNAL OF UNIVERSAL

IMPACT FACTOR 1.89***

VALUABLE INSIGHT INTO THE SYNTHESIS AND BIOLOGICAL

microwave synthesis is being practiced owing to its vitality in

organic synthesis procedures. It is very well known to all of us that

the heterocyclic compounds play a vital role in medicine,

cardiovascular, antioxidant, anti-inflammatory, anti-HIV activities

Full Text Available On www.ijupbs.com

International Standard Serial Number (ISSN): 2319-8141

troublesome hazardous waste sites that are

International Standard Serial Number (ISSN): 2319-8141

Full Text Available On www.ijupbs.com

International Standard Serial Number (ISSN): 2319-8141

Classification of fused heterocyclic compounds:

Compounds with Compounds

I) Compounds without N,O,S :

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International Standard Serial Number (ISSN): 2319-8141

II) (i) Compounds with one nitrogen:

(ii) Compounds with two nitrogens :

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International Standard Serial Number (ISSN): 2319-8141

III) (i) Compounds with one oxygen:

(ii) Compounds with 2 oxygen:

IV) Compounds with sulphur:

V) Compounds with N,O

VI) Compounds with N,S

Microwave Assisted Synthesis of Heterocyclic Compounds:

dioxide were introduced in

International Standard Serial Number (ISSN): 2319-8141

2. 2,2'-[Naphthalene-2,7-diylbis(oxy)]bis[N'-substituted acetohydrazide](6): Mix 2,2'-(naphthalene

Synthetic pathway for the preparation of compounds (6)

9, 10-dihydro-9,10-ethano- anthracene-11- carboxylic acid methyl ester: A mixture of

International Standard Serial Number (ISSN): 2319-8141

c) Coronene: Coronene (also known as superbenzene) is a polycyclic aromatic hydrocarbon (PAH)

The synthetic route of coronene

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2, 4-dimethoxyquinolines (21): Mixed well 2, 4-Dichloroquinoline (20) (1 mmol), tetrabutyl

1a, 2a R = H; 1b, 2b R = 6-CH3; 1c, 2c R = 8-CH3; 1d, 2d R = 6-OCH3; 1e, 2e R = 8-OCH3

2a, 3a R = H; 2b, 3b R = 6-CH3; 2c, 3c R = 8-CH3; 2d, 3d R = 6-OCH3; 2e, 3e R = 8-OCH3

b) Indole: Indole is an aromatic heterocyclic organic compound. It has a bicyclic structure,

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2-(4-tert-butylphenyl)-1H-indole: 4-tert-butyl-N-o-tolylbenzamide (300 mg, 1.12mmol)

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Bischler- Mohlau synthesis

MW, Tmax 1600 C

R= H, 15%, R= t-Bu, 22%

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c) Synthesis of Isoindole: Isoindole in heterocyclic chemistry is a benzo-fused pyrrole. The

iii. DDQ, 28%

2-Aryl-IH-Isoindole-l,3-Dione : A mixture of the corresponding phthalic anhydride (0.68 mmol)

Neat, 550w, 8.5 min

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Table 1: Microwave-Assisted Preparation of Substituted 9-(1, 2, 3-Triazol-1-yl) acridines

General synthetic procedure of naphtho[2,1-b]furan-1,3,4-benzotriazepines (93)

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