A Practical Procedure for the Synthesis of Esonarimod,(R, S)-2-Acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic Acid, an Antirheumatic Agent.(Part 1).

…, A Onodera, K Tomisawa, S Yokomori

Index: Noguchi, Toshiya; Onodera, Akira; Tomisawa, Kazuyuki; Yokomori, Sadakazu Chemical and pharmaceutical bulletin, 2002 , vol. 50, # 10 p. 1407 - 1412

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Citation Number: 9

Abstract

An efficient and practical procedure for the synthesis of esonarimod,(R, S)-2- acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (1), a new antirheumatic drug, has been developed. The intermediate, 2-methylene-4-(4-methylphenyl)-4-oxobutanoic acid (2), was prepared by Friedel–Crafts acylation of toluene with itaconic anhydride (3) in the presence of aluminum trichloride and nitrobenzene in 63% yield without silica gel column ...