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The Application of a Continuous Grignard Reaction in the Preparation of Fluconazole

By Korwar, Sudha; Amir, Somi; Tosso, Perrer N.; Desai, Bimbisar K.; Kong, Caleb J.; Fadnis, Swara; Telang, Nakul S.; Ahmad, Saeed; Roper, Thomas D.; Gupton, B. Frank

Published on CMKC

Abstract

The application of continuous methods in the synthesis of active pharmaceutical ingredients continues to receive significant attention in the academic as well as the industrial research communities. One of the major advantages of continuous methods is the ability to safely access kinetic synthons as well as highly reactive reagents that are typically unavailable through traditional batch methods. In this work, we report the high-yielding, clean formation of an aryl-turbo Grignard and its selective addition to a highly-enolizable 1,3-dichloroacetone, for the continuous synthesis of a key intermediate for fluconazole, a widely-prescribed anti-fungal agent. In addition, process optimization of the final API was also carried out to arrive at a semi-continuous method to this essential medicine.

Journal

European Journal of Organic Chemistry. Volume 2017, 2017, 6495-6498

DOI

10.1002/ejoc.201701002

Type of publication

Peer-reviewed journal

Affiliations

  • Virginia Commonwealth University

Article Classification

Research Article

Classification Areas

  • API

Tags