Trifluoroacetic Anhydride as Acylating Agent and Dehydrant in One-pot Synthesis of Nirmatrelvir
文献类型：期刊论文
| 作者 | Jin, Chen2,3; Zhaug, Yan3; Li, Rui2,3; Yang, Xiaojun1; Zhu, Fuqiang1; Jiang, Xiangrui3 ; Zhang, Qiumeng3; Shen, Jingshan2,3
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| 刊名 | INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY
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| 出版日期 | 2022-10-01 |
| 卷号 | 32期号:4页码:429-432 |
| ISSN号 | 0971-1627 |
| 通讯作者 | Zhang, Qiumeng(qmzhang@simm.ac.cn) |
| 英文摘要 | Nirmatrelvir is an effective ingredient in the anti COVID-19 drug Paxlovid. There were two key steps in the original synthetic route, which involved trifluoroacetylation and dehydration. A facile and efficient synthesis of nirmatrelvir is described in this work. Intermediate 7 was converted to nirmatrelvir in one-pot synthesis with trifluoroacetic anhydride. In addition, the condensation and deprotection conditions were optimized. The yield of nirmatrelvir produced from 1raised from 51.6% to 72.5%. |
| 资助项目 | Shanghai Science and Technology Committee in China[19430750100] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| 出版者 | CONNECT JOURNALS |
| WOS记录号 | WOS:000911427900003 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/303702]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhang, Qiumeng |
| 作者单位 | 1.Topharman Shanghai Co Ltd, Shanghai 201203, Peoples R China 2.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Jiangsu, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jin, Chen,Zhaug, Yan,Li, Rui,et al. Trifluoroacetic Anhydride as Acylating Agent and Dehydrant in One-pot Synthesis of Nirmatrelvir[J]. INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY,2022,32(4):429-432. |
| APA | Jin, Chen.,Zhaug, Yan.,Li, Rui.,Yang, Xiaojun.,Zhu, Fuqiang.,...&Shen, Jingshan.(2022).Trifluoroacetic Anhydride as Acylating Agent and Dehydrant in One-pot Synthesis of Nirmatrelvir.INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY,32(4),429-432. |
| MLA | Jin, Chen,et al."Trifluoroacetic Anhydride as Acylating Agent and Dehydrant in One-pot Synthesis of Nirmatrelvir".INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 32.4(2022):429-432. |
入库方式： OAI收割
来源：上海药物研究所
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