{"title":"抗covid -19药物瑞德西韦的化学合成。","authors":"Mo Wang, Lu Zhang, Xiaohong Huo, Zhenfeng Zhang, Wanbin Zhang","doi":"10.1002/cpz1.303","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":11174,"journal":{"name":"Current Protocols","volume":" ","pages":"e303"},"PeriodicalIF":0.0000,"publicationDate":"2021-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9015308/pdf/CPZ1-1-e303.pdf","citationCount":"2","resultStr":"{\"title\":\"Chemical Synthesis of the Anti-COVID-19 Drug Remdesivir.\",\"authors\":\"Mo Wang, Lu Zhang, Xiaohong Huo, Zhenfeng Zhang, Wanbin Zhang\",\"doi\":\"10.1002/cpz1.303\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":11174,\"journal\":{\"name\":\"Current Protocols\",\"volume\":\" \",\"pages\":\"e303\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2021-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9015308/pdf/CPZ1-1-e303.pdf\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Protocols\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1002/cpz1.303\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Protocols","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1002/cpz1.303","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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