"One-Pot" Synthesis of Molnupiravir from Cytidine | |
Hu, TW (Hu, Tianwen) [1] , [2]; Xie, YC (Xie, Yuanchao) [3]; Zhu, FQ (Zhu, Fuqiang) [4]; Gong, XD (Gong, Xudong) [4]; Liu, Y (Liu, Yin) [2] , [3]; Xue, HT (Xue, Haitao) [2] , [3]; Aisa, HA (Aisa, Haji A.) [1] , [2]; Shen, JS (Shen, Jingshan) [2] , [3] | |
刊名 | ORGANIC PROCESS RESEARCH & DEVELOPMENT |
2022 | |
卷号 | 26期号:2页码:358-364 |
关键词 | molnupiravir cytidine one-pot synthesis DMF-DMA |
ISSN号 | 1083-6160 |
DOI | 10.1021/acs.oprd.1c00419 |
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记录号 | WOS:000758184400014 |
内容类型 | 期刊论文 |
源URL | [http://ir.xjipc.cas.cn/handle/365002/8160] |
专题 | 新疆理化技术研究所_资源化学研究室 |
通讯作者 | Aisa, HA (Aisa, Haji A.) [1] , [2] |
作者单位 | 1.Topharman Shanghai Co Ltd, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China |
推荐引用方式 GB/T 7714 | Hu, TW ,Xie, YC ,Zhu, FQ ,et al. "One-Pot" Synthesis of Molnupiravir from Cytidine[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2022,26(2):358-364. |
APA | Hu, TW .,Xie, YC .,Zhu, FQ .,Gong, XD .,Liu, Y .,...&Shen, JS .(2022)."One-Pot" Synthesis of Molnupiravir from Cytidine.ORGANIC PROCESS RESEARCH & DEVELOPMENT,26(2),358-364. |
MLA | Hu, TW ,et al.""One-Pot" Synthesis of Molnupiravir from Cytidine".ORGANIC PROCESS RESEARCH & DEVELOPMENT 26.2(2022):358-364. |
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