A Two-step Synthesis of the Anti-cancer Drug (R,S)-Bicalutamide

Abstract

A short, efficient synthesis of the non-steroidal antiandrogen (R,S)-bicalutamide is presented. This new route generates bicalutamide in only two steps with an overall yield of 73%. The key step is a 1,2 addition of a methyl sulfone to a keto-amide.

Key words

addition reaction - aldol reaction - antiandrogen - antitumor agent - keto-amide

References

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  Overall yield was calculated from the reported yields of individual or representative reactions in the synthesis

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Chem. Abstr., 1986, 101: 54739