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6 5. A general, highly flexible Cu-catalyzed domino C-N coupling/hydroamination reaction constitutes a straightforward alternative to existing methodology for the preparation of pyrroles and pyrazoles 27 . R R' R" + NH 2 Boc 5 mol % Cul Cs 2 CO 3 THF, 80 °C, 4 - 15 h R NBoc R' R" 6. An efficient and highly versatile microwave-assisted Paal-Knorr condensation of various 1,4-diketones gave furans, pyrroles and thiophenes in good yields. In addition, transformations of the methoxycarbonyl moiety, such as Curtius rearrangement, hydrolysis to carboxylic acid, or the conversion into amine by reaction with a primary amine in the presence of Me 3 Al, are studied 28 . O CO 2 Me H 3 C CH 3 + H 2 N O R'' AcOH MW 150 W, 12 min 170 °C, open vessel R N R'' CO 2 Me R' 7. The synthesis of N-acylpyrroles from primary aromatic amides and excess 2,5- dimethoxytetrahydrofuran in presence of one equivalent of thionyl chloride offers short reaction times, mild reaction conditions, and easy workup 29 . Ar O NH 2 + O MeO OMe SOCl 2 50 or 80 °C 10 - 120 min Ar N O
7 8. Propargyl vinyl ethers and aromatic amines are effectively converted into tetraand pentasubstituted 5-methylpyrroles through a silver(I)-catalyzed propargyl- Claisen rearrangement, an amine condensation, and a gold(I)- catalyzed 5-exodig heterocyclization in a convenient one-pot process 30 . O R' R O OEt 5 mol % AGBF 4 CH 2 Cl 2 23 °C, 30 min O R' O R OEt 5 mol % (PPh 3 ) AuCl ArNH 2 38 °C, 0.5 - 4 h R' Ar N C H 3 EtO R O 9. Various 2,3,4-trisubstituted pyrroles are easily accessible in one step from readily available acetylenes and acceptor-substituted methyl isocyanides by base-mediated or copper-catalyzed cycloadditions. Scope and limitations of both pyrrole syntheses are discussed 31 . C H 3 EWG EWG NC + R EWG' base THF, 20 °C, 2 h EWG N H 10. A novel and efficient multicomponent reaction of N-tosylimines, DMAD, and isocyanides for the synthesis of 2-aminopyrrole systems was uncovered 32 . Ar NTs+ RN C: + CO 2 Me r.t., 14 - 22 h benzene Ar NTs NH CH 3 CO 2 Me MeO2C CO 2 Me
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 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
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
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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
Page 241 and 242:
236 Presentation of Paper & Confere
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