Journal
CHEMICAL SOCIETY REVIEWS
Volume 50, Issue 3, Pages 1522-1586Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0cs00196a
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Funding
- Ministry of Science and Technology of China [2019ZX09721001-008]
- National Natural Science Foundation of China [21871031, 81773889, 81630101, 81891012]
- Thousand Talents Program of Sichuan Province
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Asymmetric organocatalysis has made significant contributions to organic synthesis since the early 2000s, especially in medicinal chemistry. This review provides a comprehensive overview of the specific applications of asymmetric organocatalysis in pharmaceutical synthesis, with a focus on the synthesis strategies of various bioactive molecules and their future prospects.
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.
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