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34 C, H, N (in %): Found: 69.40 (C), 6.84 (H), 13.45 (N), Cacld: 69.43 (C), 6.80 (H), 13.49 (N) Ethyl 4-[5-(2-flourophenyl)-4, 5-dihydro-1H-pyrazol-3-yl]-3, 5-dimethyl-1Hpyrrole-2-carboxylate (VGM-11) IR (KBr) cm -1 : 3314, 3262 (-NH, str.), 1344 (-C-N, str.), 1686 (-C=O, str.), 1520 (-C=C, str. of pyrrole), 1488 (-CH 2 def.), 2940, 2916 (-CH, asym. str.), 1240 (- CH 2 , ipd.), 758 (-CH 2 , oopd.), 1089 (-C-O-C, sym, str.) C, H, N (in %): Found: 65.66 (C), 6.10(H), 12.74 (N), Cacld: 65.64 (C), 6.12 (H), 12.76 (N) Ethyl 4-[5-(2-methoxyphenyl)-4, 5-dihydro-1H-pyrazol-3-yl]-3, 5-dimethyl-1Hpyrrole-2-carboxylate (VGM-12) IR (KBr) cm -1 : 3267, 3186 (-NH, str.), 1390 (-C-N, str.), 1689 (-C=O, str.), 1514 (-C=C, str. of pyrrole), 1490 (-CH 2 def.), 1432 (-CH 3 , C-H def.), 2965 (-CH, asym. str. ), 1244 (-CH 2 , ipd.), 775 (-CH 2 , oopd.), 1010-1024 (-C-O-C, sym, str.) C, H, N (in %): Found: 66.82 (C), 6.82(H), 12.28 (N), Cacld: 66.84 (C), 6.79 (H), 12.31 (N) Ethyl 4-[5-(3-chlorophenyl)-4, 5-dihydro-1H-pyrazol-3-yl]-3, 5-dimethyl-1Hpyrrole-2-carboxylate (VGM-13) IR (KBr) cm -1 : 3326, 3240 (-NH, str.), 1364 (-C-N, str.), 1688 (-C=O, str.), 1521 (-C=C, str. of pyrrole), 1490 (-CH 2 def.), 2940, 2911 (-CH, asym. str.), 1238 (- CH 2 , ipd.), 784 (-CH 2 , oopd.), 1080-1040 (-C-O-C, sym, str.) C, H, N (in %): Found: 62.54 (C), 5.80 (H), 10.22 (N), Cacld: 62.52 (C), 5.83 (H), 10.25 (N) Ethyl 4-[5-(2-hydroxycyclohexa-2, 5-dien-1-yl)-4, 5-dihydro-1H-pyrazol-3-yl]- 3, 5-dimethyl-1H-pyrrole-2-carboxylate (VGM-14) IR (KBr) cm -1 : 3586 (-OH, str, ) 3246, 3174 (-NH, str.), 1541 (-NH, def.), 1387 (- C-N, str.), 1688 (-C=O, str.), 1524 (-C=C, str. of pyrrole), 1474 (-CH 2 def.), 1423 (-CH 3 , C-H def.), 2954 (-CH, asym. str. ), 2864, 2812 (-CH, sym. str.), 1240 (- CH 2 , ipd.), 784 (-CH 2 , oopd.), 1010-1098 (-C-O-C, sym, str.) C, H, N (in %): Found: 66.02 (C), 6.49 (H), 12.80 (N), Cacld: 66.04 (C), 6.47 (H), 12.84 (N) Ethyl 4-[5-(3-flourophenyl)-4, 5-dihydro-1H-pyrazol-3-yl]-3, 5-dimethyl-1Hpyrrole-2-carboxylate (VGM-15)
35 IR (KBr) cm -1 : 3320, 3246 (-NH, str.), 1340 (-C-N, str.), 1680 (-C=O, str.), 1516 (-C=C, str. of pyrrole), 1480 (-CH 2 def.), 2974, 2910 (-CH, asym. str.), 1242 (- CH 2 , ipd.), 762 (-CH 2 , oopd.), 1080-1014 (-C-O-C, sym, str.) C, H, N (in %): Found: 65.67 (C), 6.10 (H), 12.73 (N), Cacld: 65.64 (C), 6.12 (H), 12.76 (N) Ethyl 4-[5-(4-hydroxycyclohexa-2, 5-dien-1-yl)-4, 5-dihydro-1H-pyrazol-3-yl]- 3, 5-dimethyl-1H-pyrrole-2-carboxylate (VGM-16) IR (KBr) cm -1 : 3574 (-OH, str, ) 3346, 3214 (-NH, str.), 1380 (-C-N, str.), 1691 (- C=O, str.), 1520 (-C=C, str. of pyrrole), 1470 (-CH 2 def.), 1432 (-CH 3 , C-H def.), 3014 (Ar-CH,str.) 2948 (-CH, asym. str. ), 2874, (-CH, sym. str.), 1248 (-CH 2 , ipd.), 781 (-CH 2 , oopd.), 1098-1012 (-C-O-C, sym, str.) C, H, N (in %): Found: 66.05 (C), 6.45 (H), 12.82 (N), Calcld: 66.04 (C), 6.47 (H), 12.84 (N) Ethyl 4-[5-(4-naphthalene)-4, 5-dihydro-1H-pyrazol-3-yl]-3, 5-dimethyl-1Hpyrrole-2-carboxylate (VGM-17) IR (KBr) cm -1 : 3318, 3240 (-NH, str.), 1538 (-NH, def.), 1392 (-C-N, str.), 1679 (-C=O, str.), 1521 (-C=C, str. of pyrrole), 1490 (-CH 2 def.), 1420 (-CH 3 , C-H def.), 3014 (Ar-CH, str.) 2964, 2910 (-CH, asym. str. ), 2864 (-CH, sym. str.), 1242 (- CH 2 , ipd.), 784 (-CH 2 , oopd.), 1088-1014 (-C-O-C, sym, str.) C, H, N (in %): Found: 72.72 (C), 6.90 (H), 11.54 (N), Cacld: 72.70 (C), 6.93 (H), 11.56 (N) Ethyl 4-[5-(3-hydroxycyclohexa-2, 5-dien-1-yl)-4, 5-dihydro-1H-pyrazol-3-yl]- 3, 5-dimethyl-1H-pyrrole-2-carboxylate (VGM-18) IR (KBr) cm -1 : 3574 (-OH, str, ) 3346, 3214 (-NH, str.), 1540 (-NH, def.), 1384 (- C-N, str.), 1690 (-C=O, str.), 1531 (-C=C, str. of pyrrole), 1470 (-CH 2 def.), 1430 (-CH 3 , C-H def.), 2917 (-CH, asym. str.), 2874, 2810 (-CH, sym. str.), 1244 (-CH 2 , ipd.), 788 (-CH 2 , oopd.), 1098-1024 (-C-O-C, sym, str.) C, H, N (in %): Found: 66.02 (C), 6.49 (H), 12.81 (N), Cacld: 66.04 (C), 6.47 (H), 12.84 (N)
Page 1 and 2: Saurashtra University Re - Accredit
Page 3 and 4: Statement under O.Ph.D.7 of Saurash
Page 5 and 6: To My Family, With Love
Page 7 and 8: I would like to thank my dear lab m
Page 9 and 10: Synthetic Aspects 55 QSAR Study 59
Page 11 and 12: CHAPTER-6 MICROWAVE ASSISTED SYNTHE
Page 13: Chapter-1 Introduction, Synthesis a
Page 16 and 17: 2 Their biological functions are as
Page 18 and 19: 4 5. The reaction of β-amino-α,
Page 20 and 21: 6 5. A general, highly flexible Cu-
Page 22 and 23: 8 11. A new microwave-assisted rear
Page 24 and 25: 10 Gaetano Dattolo 38 and his resea
Page 26 and 27: 12 -CONHOCH 3 O -CONHNH 2 Cl C N F
Page 28 and 29: 14 Molecular modeling and docking c
Page 30 and 31: 16 R 3 R 4 R 1 ,R 2 ,R 3 ,=H, alkyl
Page 32 and 33: 18 CH 3 CH 3 N C O NH H 3 CH 3 F N
Page 34 and 35: 20 Drug Name Chemical Structure : :
Page 36 and 37: 22 1.3 REACTION SCHEMES 1.3.1 Schem
Page 38 and 39: 24 1.4 Experimental Protocols Comme
Page 41 and 42: 27 1.7 SPECTRAL ANALYSIS 1.7.1 IR S
Page 43 and 44: 29 of phenyl ring from molecule, ba
Page 45 and 46: 31 Ethyl 3,5-dimethyl-4-[5-(3-nitro
Page 47: 33 C, H, N (in %): Found: 60.62(C),
Page 51 and 52: IR spectrum of Ethyl 4-[5-(4-methox
Page 53 and 54: 39 1 H NMR spectrum of Ethyl 3, 5-d
Page 55 and 56: 41 1 H NMR spectrum of Ethyl 3, 5-d
Page 57 and 58: Mass spectrum of Ethyl 3, 5-dimethy
Page 59 and 60: 45 Mass spectrum of Ethyl 3, 5-dime
Page 61 and 62: 47 29. Ekkati A. R., Bates D. K., S
Page 63 and 64: Chapter-2 Introduction, Synthesis a
Page 65 and 66: 50 with improved bioavailability, t
Page 67 and 68: 52 combining Ca 2+ antagonism and t
Page 69 and 70: 54 alpha1G, expressed in Xenopus oo
Page 71 and 72: 56 3,5-Dibenzoyl-4-(3-phenoxyphenyl
Page 73 and 74: 58 PAF, will have clinical utilitie
Page 75 and 76: 60 According to the 3D QSAR study,
Page 77 and 78: 62 2.3.3 Scheme 3 O O R HN CH 3 O H
Page 79 and 80: 64 2.5 EXPERIMENTAL 2.5.1 N-(naphth
Page 81 and 82: 66 2.6 PHYSICAL DATA TABLE 2.6.1 Ph
Page 83 and 84: 68 2.7 SPECTRAL DISCUSSION 2.7.1 IR
Page 85 and 86: 70 ionization chamber and resolved
Page 87 and 88: 72 C, H, N (in %): Found: 78.10 (C)
Page 89 and 90: 74 1,4- Dihydro -4- (4-hydroxy phen
Page 91 and 92: 76 C, H, N (in %): Found: 69.87 (C)
Page 93 and 94: IR spectrum of 1,4- dihydro-4-(4-me
Page 95 and 96: 1 H NMR spectrum of 1,4- dihydro-4-
Page 97 and 98: 1 H NMR spectrum of 1,4- dihydro-4-
Page 99 and 100:
84 REFERENCES 1. Alker, D.; Arrowsm
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86 51. Pickard, J. D.; Murray, G. D
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Chapter - 3 A mini review of Dihydr
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urea, is the first intermediate in
Page 107 and 108:
91 A variety of substituted aromati
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93 first organocatalytic asymmetric
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95 one system in high yield and hig
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97 classical dihydropyridine calciu
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99 Atwal et al 58 examined a series
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101 biological activity. Biological
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103 Applying intramolecular Heck re
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105 furo[3,4-d]pyrimidines, pyrrolo
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107 Figure 2: The reaction of 2-ami
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109 O O O R 1 NH ClCH 2 COOH R 1 N
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111 A N B N O S R 1 3.6 Biginelli R
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113 3.7.1 Name reactions Following
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115 and urea or thiourea to afford
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117 3.8.1 Cycloaddition reaction Re
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119 3.8.5 Solid Phase Organic Synth
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121 Lusch and Tallarico 31 reported
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123 continuation of this work, it w
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124 INTRODUCTION A general introduc
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126 4.1.2 Scheme-2 R 2 O R 1 NH NH
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128 4.1.5 Reaction Mechanism O NH N
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130 4.3.2 N - (Substituted phenyl)-
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132 13. AKS- 562 4-F 2,3,5,6- 441.5
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134 14 AKS-583 4-F 3-OCH 3 397.46 1
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136 4.5 SPECTRAL ANALYSIS Spectral
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gave multiplet signal at similar re
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140 IR(KBr)cm -1 :3192 (-NH,str),31
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142 N - (4-Fluoro phenyl) -5- (3-me
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144 Mass: 435 (2), 431 (10), 416 (3
Page 163 and 164:
IR spectrum of N,6-Bis(4-chlorophen
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1 H NMR Spectrum of 5-(2-Chlorophen
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150 1 H NMR Spectrum of N-(4-Chloro
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152 1 H NMR Spectrum of N,6-Bis(1-n
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Mass Spectrum of N-(4-Chlorophenyl)
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Mass Spectrum of 5-(2-Chlorophenyl)
Page 175 and 176:
Chapter-5 Synthesis and Characteriz
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159 5.1 REACTOIN SCHEMES 5.1.1 Sche
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161 5.2 Experimental 5.2.1 N-Substi
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163 5.3 PHYSICAL DATA 5.3.1 Physica
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165 AKS-916 2,4diCH 3 4-Cl 3,4,5-tr
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167 The supplementary characterizat
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169 IR(KBr,cm -1 ): 3292-3228 (-NH)
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171 IR(KBr,cm -1 ): 3312-3215 (-NH)
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173 N-(2,4-Di-methylphenyl)-N-(4-ch
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IR spectrum of 4-(phenyl)-N-(4-chlo
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IR spectrum of 4-(4-flourophenyl)-N
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1 H NMR spectrum of 4-(4-hydroxyphe
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1 H NMR spectrum of N-(3-methylphen
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Mass spectrum of 4-(2,3-benzophenyl
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184 INTRODUCTION The current chapte
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186 6.1.3 Scheme-3 CH 3 R NH O H 3
Page 207 and 208:
188 6.2 EXPERIMENTAL N- (Substitute
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190 6.3.2 Physical data of 6-methyl
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192 at 7.59 δ ppm with J value 8.8
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194 N-(4-Flourophenyl)-6-methyl-2-o
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196 C, H, N (in %): Found: 71.72 (C
Page 217 and 218:
198 C, H, N (in %): Found: 68.09 (C
Page 219 and 220:
IR spectrum of N-( 4-Flouro phenyl)
Page 221 and 222:
1 H NMR spectrum of N-(4-Fluorophen
Page 223 and 224:
Mass spectrum of N-(2,3-Dimethylphe
Page 225 and 226:
206 References 1. Kappe, C. O.; Acc
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208 54. Forray, C.; Bard, J. A.; We
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210 96. Manhi, M. and Abdel-Fattah,
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212 153. Trost, B. M.; Crawley, M.
Page 233 and 234:
213 Biological Activity Study The p
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215 Incubation time and temperature
Page 237 and 238:
217 34. AKS-904 -- - - - 100 100 35
Page 239 and 240:
234 SUMMARY OF WORK The work presen
Page 241 and 242:
236 Presentation of Paper & Confere
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