Issue 17, 2021

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

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.

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

Article information

Article type
Critical Review
Submitted
07 may 2021
Accepted
03 avq 2021
First published
03 avq 2021
This article is Open Access
Creative Commons BY license

Green Chem., 2021,23, 6117-6138

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

S. B. Ötvös and C. O. Kappe, Green Chem., 2021, 23, 6117 DOI: 10.1039/D1GC01615F

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements