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Short Paper | Special issue | Vol 88, No. 2, 2014, pp.1655-1660
Published online, 8th November, 2013
DOI: 10.3987/COM-13-S(S)120
Improved Synthesis of Antipsychotic Drug Bifeprunox

Gerhard Laus, Sven Nerdinger,* Volker Kahlenberg, and Herwig Schottenberger

*Sandoz GmbH, Biochemiestrasse 10, 6250 Kundl , Austria

Abstract

A new and efficient six-step synthesis of the antipsychotic drug bifeprunox is reported. The key step is azidation of a lithiated phenol ether. Subsequent reduction of the azide, removal of phenol protecting group, and cyclization lead to the desired benzoxazolinone.