Development of a synthesis for a long-term oxazolidinone antibacterial

A Choy, N Colbry, C Huber, M Pamment…

Index: Choy, Allison; Colbry, Norman; Huber, Christian; Pamment, Michael; Van Duine, Justin Organic Process Research and Development, 2008 , vol. 12, # 5 p. 884 - 887

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Citation Number: 15

Abstract

Linezolid, compound 1, is a member of the oxazolidinone class of antibacterials and has had recent clinical interest due to its potential use as a long-term treatment for bacterial infection. Detailed herein are improvements to the original synthesis to enable phase I clinical trials. Of particular interest is the preparation of a key oxindole subunit utilizing a Pd- mediated cyclization. Optimization of the synthesis of the oxindole included the use of ...