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Large-Scale Applications of Amide Coupling Reagents for the Synthesis of Pharmaceuticals

Joshua R. Dunetz^*†, Javier Magano^*‡, and Gerald A. Weisenburger^*‡

^† Process Chemistry, Gilead Sciences, 333 Lakeside Drive, Foster City, California 94404, United States

^‡ Chemical Research & Development, Pfizer Worldwide Research & Development, Eastern Point Road, Groton, Connecticut 06340, United States

Org. Process Res. Dev., 2016, 20 (2), pp 140–177

DOI: 10.1021/op500305s

Publication Date (Web): November 15, 2015

Copyright © 2015 American Chemical Society

*E-mail: Joshua.Dunetz@Gilead.com., *E-mail: Javier.Magano@Pfizer.com., *E-mail: Gerald.A.Weisenburger@Pfizer.com.

Abstract

 

 

 

This review showcases various coupling reagents which have been implemented specifically for large-scale amide synthesis via the condensation of an acid and amine, while highlighting the benefits and drawbacks of each reagent on an industrial scale.

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Received 20 September 2014

Published online 15 November 2015

Published in print 19 February 2016

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