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Seven-Step Continuous Flow Synthesis of Linezolid Without Intermediate Purification

By Russel, M. Grace; Jamison, Timothy F.

Published on CMKC

Abstract

Herein, the blockbuster antibacterial drug linezolid is synthesized from simple starting blocks by a convergent continuous flow sequence involving seven (7) chemical transformations. This is the highest total number of distinct reaction steps ever performed in continuous flow without conducting solvent exchanges or intermediate purification. Linezolid was obtained in 73 % isolated yield in a total residence time of 27 minutes, corresponding to a throughput of 816 mg h−1.

Journal

Angewandte Chemie International Edition. Volume 58, 2019, 7678-7681

DOI

10.1002/anie.201901814

Type of publication

Peer-reviewed journal

Affiliations

  • Massachusetts Institute of Technology

Article Classification

Research Article

Classification Areas

  • API

Tags