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Synthesis 2002(7): 0850-0852
DOI: 10.1055/s-2002-28508
SHORTPAPER
© Georg Thieme Verlag Stuttgart · New York

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

Kenneth D. James*, Nnochiri N. Ekwuribe
Department of Innovation, Nobex Corporation, 617 Davis Drive; Durham, NC 27713, USA
Fax: +1(919)4749407; e-Mail: kjames@nobexcorp.com; e-Mail: nekwuribe@nobexcorp.com;
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Publication History

Received 3 February 2002
Publication Date:
14 May 2002 (online)

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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

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