Friedel-Crafts acylation for synthesis of aryl and heteroaryl-(3-ethyl-4-nitro-phenyl)-methanones

摘要

Synthesis process comprises: (a) reacting 3-ethyl-4-nitrobenzoic acid with a thionyl halide to produce a 3-ethyl-4-nitrobenzoic acid halide; and (b) Friedel-Crafts acylation by reacting the 3-ethyl-4-nitrobenzoic acid chloride or the 3-ethyl-4-nitrobenzoic acid anhydride with an optionally substituted aryl-H to form an optionally substituted (3-ethyl-4-nitro-phenyl)-aryl-methanone. Independent claims are included for: (1) the (3-ethyl-4-nitrophenyl)-aryl-methanone or [3-(2-hydroxy-1-methyl-ethyl)-4-nitrophenyl]-aryl-methanone, where the aryl is a condensed aromate, which is optionally substituted; and (2) a nucleoside containing a substituent at the 5' or 3' position, where the substituent is a [3-(2-O-1-methyl-ethyl)-4-nitrophenyl]-aryl-methanone.