AbstractRemdesivir 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‐4Basic Protocol 2: Synthesis of chiral bicyclic imidazole Ad‐DPIBasic Protocol 3: Synthesis of remdesivir

中文翻译：

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抗COVID-19药物瑞德西韦的化学合成

摘要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，磷‐外消旋磷酰氯的合成过程很简单。然后，通过有机催化对受保护的核苷GS441524进行不对称磷酸化，可以得到受保护的瑞德西韦磷‐手性双环咪唑催化的外消旋磷酰氯。最后，瑞德西韦可以通过脱保护轻松制备。© 2021 Wiley 期刊有限责任公司。基本协议1：2-乙基丁基（氯（苯氧基）磷酰基）-的合成L丙氨酸盐拉克‐4基本协议2: 手性双环咪唑的合成广告-DPI基本协议3: 瑞德西韦的合成