Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, Frontiers Science Center for Transformative Molecules, School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai, China.
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
Curr Protoc. 2021 Dec;1(12):e303. doi: 10.1002/cpz1.303.
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.
瑞德西韦已成为治疗 COVID-19 的重要化合物。在这里，我们描述了这种抗 COVID-19 药物的催化不对称合成。首先，通过简便的方法合成 P-外消旋磷酰氯。然后，通过手性双环咪唑催化的 P-外消旋磷酰氯对保护的核苷 GS441524 的有机催化不对称磷酸化反应，有可能获得保护的瑞德西韦。最后，通过脱保护很容易制备瑞德西韦。© 2021 年威利父子公司。基础方案 1：2-乙基丁基（氯（苯氧基）膦酰基）-L-丙氨酸 rac-4 的合成基础方案 2：手性双环咪唑 Ad-DPI 的合成基础方案 3：瑞德西韦的合成。
