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Issue 3, 2021
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Asymmetric organocatalysis: an enabling technology for medicinal chemistry

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Abstract

The efficacy and synthetic versatility of asymmetric organocatalysis have contributed enormously to the field of organic synthesis since the early 2000s. As asymmetric organocatalytic methods mature, they have extended beyond the academia and undergone scale-up for the production of chiral drugs, natural products, and enantiomerically enriched bioactive molecules. This review provides a comprehensive overview of the applications of asymmetric organocatalysis in medicinal chemistry. A general picture of asymmetric organocatalytic strategies in medicinal chemistry is firstly presented, and the specific applications of these strategies in pharmaceutical synthesis are systematically described, with a focus on the preparation of antiviral, anticancer, neuroprotective, cardiovascular, antibacterial, and antiparasitic agents, as well as several miscellaneous bioactive agents. The review concludes with a discussion of the challenges, limitations and future prospects for organocatalytic asymmetric synthesis of medicinally valuable compounds.

Graphical abstract: Asymmetric organocatalysis: an enabling technology for medicinal chemistry

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Article information


Submitted
31 Aug 2020
First published
26 Jan 2021

Chem. Soc. Rev., 2021,50, 1522-1586
Article type
Review Article

Asymmetric organocatalysis: an enabling technology for medicinal chemistry

B. Han, X. He, Y. Liu, G. He, C. Peng and J. Li, Chem. Soc. Rev., 2021, 50, 1522
DOI: 10.1039/D0CS00196A

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