中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
"One-Pot" Synthesis of Molnupiravir from Cytidine

文献类型：期刊论文

作者Hu, Tianwen2,3; Xie, Yuanchao1; Zhu, Fuqiang4; Gong, Xudong4; Liu, Yin1,3; Xue, Haitao1,3; Aisa, Haji A.2,3; Shen, Jingshan1,3
刊名ORGANIC PROCESS RESEARCH & DEVELOPMENT
出版日期2022-02-18
卷号26期号:2页码:358-364
关键词molnupiravir cytidine one-pot synthesis DMF-DMA
ISSN号1083-6160
DOI10.1021/acs.oprd.1c00419
通讯作者Aisa, Haji A.(haji@ms.xjb.ac.cn) ; Shen, Jingshan(shenjingshan@simm.ac.cn)
英文摘要A one-pot process for preparing molnupiravir from cytidine was developed. The advantages of this synthesis were as follows: (1) The presence of N,N-dimethylformamide dimethyl acetal (DMF-DMA) facilitated the selective protection of 2 ',3 '- dihydroxyls and amino of cytidine, which eliminated the negative impact of these groups on the following isobutyrylation at 5 '- hydroxyl. (2) Degradations of the product in the deprotection stage were avoided since a mild condition was used. (3) The achievement of deprotection and hydroxyamination in one single step improved the synthetic efficiency. (4) Molnupiravir with high purity (purity up to 99.7% analyzed by high-performance liquid chromatography (HPLC)) was obtained in a yield of 63% through crystallization.
WOS关键词EIDD-2801 ; MK-4482
资助项目Shanghai Municipal Science and Technology Major Project ; Shanghai Science and Technology Committee in China[21S11903100]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000758184400014
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/300327]  
专题中国科学院上海药物研究所
通讯作者Aisa, Haji A.; Shen, Jingshan
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
4.Topharman Shanghai Co Ltd, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Hu, Tianwen,Xie, Yuanchao,Zhu, Fuqiang,et al. "One-Pot" Synthesis of Molnupiravir from Cytidine[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2022,26(2):358-364.
APA Hu, Tianwen.,Xie, Yuanchao.,Zhu, Fuqiang.,Gong, Xudong.,Liu, Yin.,...&Shen, Jingshan.(2022)."One-Pot" Synthesis of Molnupiravir from Cytidine.ORGANIC PROCESS RESEARCH & DEVELOPMENT,26(2),358-364.
MLA Hu, Tianwen,et al.""One-Pot" Synthesis of Molnupiravir from Cytidine".ORGANIC PROCESS RESEARCH & DEVELOPMENT 26.2(2022):358-364.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。