Chemical Synthesis of the Anti-COVID-19 Drug Remdesivir

被引：3
|
作者：
Wang, Mo [1 ,2 ]
Zhang, Lu [2 ]
Huo, Xiaohong [1 ]
Zhang, Zhenfeng [2 ]
Zhang, Wanbin [1 ,2 ]
机构：
[1] Shanghai Jiao Tong Univ, Sch Chem & Chem Engn, Frontiers Sci Ctr Transformat Mol, Shanghai Key Lab Mol Engn Chiral Drugs, Shanghai, Peoples R China
[2] Shanghai Jiao Tong Univ, Sch Pharm, Shanghai, Peoples R China
来源：
CURRENT PROTOCOLS | 2021年 / 1卷 / 12期
基金：
国家重点研发计划; 中国国家自然科学基金;
关键词：
anti-COVID-19; drug; asymmetric phosphorylation; chiral bicyclic imidazole; organocatalysis; ENANTIOSELECTIVE C-ACYLATION; KINETIC RESOLUTION; GS-5734; DESIGN; EBOLA;
D O I：
10.1002/cpz1.303
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
Remdesivir has become an important compound for the treatment of COVID-19. Here, we describe the catalytic asymmetric synthesis of this anti-COVID-19 drug. First, the P-racemic phosphoryl chloride is synthesized in a facile procedure. Then, it is possible to obtain the protected remdesivir via the organocatalytic asymmetric phosphorylation of protected nucleoside GS441524 with P-racemic phosphoryl chloride catalyzed by chiral bicyclic imidazole. Finally, remdesivir is easily prepared by deprotection. (c) 2021 Wiley Periodicals LLC.
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页数：10
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