State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.
State Key Laboratory of Biotherapy and Cancer Centre, West China Hospital, Sichuan University, Chengdu 610041, China.
Chem Soc Rev. 2021 Feb 15;50(3):1522-1586. doi: 10.1039/d0cs00196a.
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.
自 21 世纪初以来，不对称有机催化的功效和综合多功能性极大地推动了有机合成领域的发展。随着不对称有机催化方法的成熟，它们已经超越了学术界，并进行了扩大规模，以生产手性药物、天然产物和对映体富集的生物活性分子。本综述全面概述了不对称有机催化在药物化学中的应用。首先呈现了药物化学中不对称有机催化策略的总体情况，并系统地描述了这些策略在药物合成中的具体应用，重点是制备抗病毒、抗癌、神经保护、心血管、抗菌和抗寄生虫药物以及几种杂生物活性药物。该综述最后讨论了手性药物合成中有机催化不对称合成的挑战、限制和未来前景。
