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CONTENTS CHAPTER 1 INTRODUCTION, SYNTHESIS AND CHARACTERIZATION OF SUBSTITUTED ETHYL 3, 5-DIMETHYL-4-[5-(PHENYL)-4,5-DIHYDRO-1H-PYRAZOL-3-YL]-1H- PYRROLE-2-CARBOXYLATE DERIVATIVES. Introduction 01 Different methods for synthesis of pyrrole 02 Recent literature survey 04 Biological profile 09 New drugs molecule introduce under clinical trials 18 Synthetic aspects 21 Reaction Scheme 22 Reaction Mechanism 23 Experimental 24 Physical Data table 26 Spectral Analysis 27 Mass Fragmentation 29 Spectral Data 30 IR Spectra 36 1 H NMR Spectral 38 Mass Spectra 42 References 46 CHAPTER-2 INTRODUCTION, SYNTHESIS AND CHARACTERIZATION OF SOME SYMMETRIC AND UNSYMMETRICAL DIHYDROPYRIMIDINE DERIVATIVES CONTAINING NAPHTHYL RING. Biological Profile 49 Recent Literature Survey 54
Synthetic Aspects 55 QSAR Study 59 Reaction Scheme 61 Experimental Observation 63 Experimental 64 Physical Data table 66 Spectral Analysis 68 Mass Fragmentation 71 Spectral Data 71 IR Spectra 78 1 H NMR Spectra 80 Mass Spectra 83 References 84 CHAPTER 3 A MINI REVIEW OF DIHYDROPYRIMIDINE DERIVATIVES Biginelli reaction 88 Literature Survey 90 Ionic liquid 96 N 3 Acylated dihydropyrimidines 101 Heck Cyclization 102 Thiazines Schaffolds 105 Microwave Assisted Synthesis 111 Name Reaction 113 Rearrangement 116 Solid Phase Synthesis 119 Synthetic Aspects 121
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: I would like to thank my dear lab m
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 and 48: 33 C, H, N (in %): Found: 60.62(C),
Page 49 and 50: 35 IR (KBr) cm -1 : 3320, 3246 (-NH
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
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45 Mass spectrum of Ethyl 3, 5-dime
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47 29. Ekkati A. R., Bates D. K., S
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Chapter-2 Introduction, Synthesis a
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50 with improved bioavailability, t
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52 combining Ca 2+ antagonism and t
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54 alpha1G, expressed in Xenopus oo
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56 3,5-Dibenzoyl-4-(3-phenoxyphenyl
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58 PAF, will have clinical utilitie
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60 According to the 3D QSAR study,
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62 2.3.3 Scheme 3 O O R HN CH 3 O H
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64 2.5 EXPERIMENTAL 2.5.1 N-(naphth
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66 2.6 PHYSICAL DATA TABLE 2.6.1 Ph
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68 2.7 SPECTRAL DISCUSSION 2.7.1 IR
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70 ionization chamber and resolved
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72 C, H, N (in %): Found: 78.10 (C)
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74 1,4- Dihydro -4- (4-hydroxy phen
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76 C, H, N (in %): Found: 69.87 (C)
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IR spectrum of 1,4- dihydro-4-(4-me
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1 H NMR spectrum of 1,4- dihydro-4-
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1 H NMR spectrum of 1,4- dihydro-4-
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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
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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
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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)
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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
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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
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198 C, H, N (in %): Found: 68.09 (C
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IR spectrum of N-( 4-Flouro phenyl)
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1 H NMR spectrum of N-(4-Fluorophen
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Mass spectrum of N-(2,3-Dimethylphe
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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.
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213 Biological Activity Study The p
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215 Incubation time and temperature
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217 34. AKS-904 -- - - - 100 100 35
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234 SUMMARY OF WORK The work presen
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236 Presentation of Paper & Confere
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