Chemical Synthesis of the Anti‐COVID‐19 Drug Remdesivir. Issue 12 (8th December 2021)

• Record Type: Journal Article
• Authors: Wang, Mo; Zhang, Lu; Huo, Xiaohong; Zhang, Zhenfeng; Zhang, Wanbin
• Is Part Of: Current protocols. Volume 1:Issue 12(2021)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2021-12-08
• Subjects: anti‐COVID‐19 drug -- asymmetric phosphorylation -- chiral bicyclic imidazole -- organocatalysis; Life sciences -- Laboratory manuals -- Periodicals; Biology -- Laboratory manuals -- Periodicals; Life sciences -- Technique -- Periodicals; Biology -- Technique -- Periodicals; 570.028
• DOI: 10.1002/cpz1.303
• Languages: English
• ISSNs: 2691-1299

Abstract

Abstract: 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. © 2021 Wiley Periodicals LLC. Basic Protocol 1 : Synthesis of 2‐ethylbutyl (chloro(phenoxy)phosphoryl)‐L ‐alaninate rac ‐4 Basic Protocol 2 : Synthesis of chiral bicyclic imidazole Ad‐DPI Basic Protocol 3 : Synthesis of remdesivir