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3.22.241.60

Continuous flow asymmetric synthesis of chiral active pharmaceutical ingredients and their advanced intermediates

By Otvos, SB; Kappe, CO

Published on CMKC

Abstract

Catalytic enantioselective transformations provide well-established and direct access to stereogenic synthons that are broadly distributed among active pharmaceutical ingredients (APIs). These reactions have been demonstrated to benefit considerably from the merits of continuous processing and microreactor technology. Over the past few years, continuous flow enantioselective catalysis has grown into a mature field and has found diverse applications in asymmetric synthesis of pharmaceutically active substances. The present review therefore surveys flow chemistry-based approaches for the synthesis of chiral APIs and their advanced stereogenic intermediates, covering the utilization of biocatalysis, organometallic catalysis and metal-free organocatalysis to introduce asymmetry in continuously operated systems. Single-step processes, interrupted multistep flow syntheses, combined batch/flow processes and uninterrupted one-flow syntheses are discussed herein.

Journal

Green Chemistry. Volume 23, 2021, 6117-6138

DOI

10.1039/d1gc01615f

Type of publication

Peer-reviewed journal

Affiliations

  • Karl Franzens University Graz
  • Res Ctr Pharmaceut Engn GmbH (RCPE)

Article Classification

Review article

Classification Areas

  • API

Tags