Convergent synthesis of the quinolone substructure of BILN 2061 via carbonylative Sonogashira coupling/cyclization.

J Org Chem

Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Rd., P.O. Box 368, Ridgefield, Connecticut 06877-0368, USA.

Published: June 2006

A convergent synthesis of quinolone 2 (key substructure of the protease inhibitor BILN 2061) was developed via palladium-catalyzed carbonylation of 2-iodo-5-methoxyaniline (4) with thiazolylacetylene 5.

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http://dx.doi.org/10.1021/jo060556qDOI Listing

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