Medicinal Chemistry
APPENDIX 3.1: BASIC REACTIONS FOR DRUG MOLECULE SYNTHESIS A. Building Blocks for the Framework Structure: C-C, C=C, C≡C, and C-H ...
DESIGNING DRUG MOLECULES TO FIT RECEPTORS 167 Conjugate addition to an α,β-unsaturated carbonyl group Cope rearrangement Diels– ...
168 MEDICINAL CHEMISTRY Michael reaction SN2 displacement by cyanide SN2 displacement by acetylide anion Aldol condensation Cat ...
DESIGNING DRUG MOLECULES TO FIT RECEPTORS 169 Dissolving metal reduction of an alkyne Hoffman elimination Reductive elimination ...
170 MEDICINAL CHEMISTRY Catalytic hydrogenation of an alkene (or alkyne) Clemmensen reduction Decarboxylation of a β-ketoacid D ...
DESIGNING DRUG MOLECULES TO FIT RECEPTORS 171 Addition of X 2 Bromination of an alkene Chlorination of an alkene Conversion of ...
172 MEDICINAL CHEMISTRY α-Halogenation of a ketone Hell–Volhard–Zelinski reaction Aldol reaction Cannizzaro reaction Cyanohydri ...
DESIGNING DRUG MOLECULES TO FIT RECEPTORS 173 Grignard reaction of an ester Hydration of an alkene (Markovnikov regiochemistry) ...
174 MEDICINAL CHEMISTRY Nucleophilic opening of an epoxide Oxymercuration–demercuration (Markovnikov regiochemistry) Cyanohydri ...
DESIGNING DRUG MOLECULES TO FIT RECEPTORS 175 Gabriel synthesis Hoffmann rearrangement Lithium aluminum hydride reduction of an ...
176 MEDICINAL CHEMISTRY Claisen rearrangement Chromate oxidation of a secondary alcohol Freidel–Crafts acylation Hydrolysis of ...
DESIGNING DRUG MOLECULES TO FIT RECEPTORS 177 Oxidation of a primary alcohol Ozonolysis of an alkene Pinacol rearrangement Benz ...
178 MEDICINAL CHEMISTRY Hydrolysis of a nitrile Iodoform reaction Oxidation of a primary alcohol Oxidation of an aldehyde Perma ...
DESIGNING DRUG MOLECULES TO FIT RECEPTORS 179 Esterification of a carboxylic acid Transesterification Treatment of an acid with ...
180 MEDICINAL CHEMISTRY Williamson ether synthesis Clemmensen reduction or Wolff–Kishner reduction Cyanation via diazomium ion ...
DESIGNING DRUG MOLECULES TO FIT RECEPTORS 181 Reduction of nitro groups Nitration Oxidation of alkyl group Sulfonation 96. Nucl ...
182 MEDICINAL CHEMISTRY Enamine formation Imine formation Ketal (acetal) formation ...
II BIOCHEMICAL CONSIDERATIONS IN DRUG DESIGN From Druggable Targets to Diseases ...
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185 Introduction to Part II Part I described the basics of medicinal chemistry and drug design. These principles follow three ba ...
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