Improved Synthesis of Key Intermediate of Baloxavir Marboxil, an Anti-Influenza Drug
文献类型：期刊论文
| 作者 | Hu, Zhenfei1,2; Li, Maocheng1; Meng, Xin1; Guo, Bin1
|
| 刊名 | CHEMISTRYSELECT
 |
| 出版日期 | 2022-08-05 |
| 卷号 | 7期号:29页码:5 |
| 关键词 | antiviral agents key intermediate process research synthesis design |
| ISSN号 | 2365-6549 |
| DOI | 10.1002/slct.202200832 |
| 通讯作者 | Guo, Bin(guobin@simm.ac.cn) |
| 英文摘要 | In this article, a process to prepare the key chiral intermediate (R)-7-(benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4c]pyrido[2,1-f][1,2,4]triazine-6,8-dione 6-R of influenza antiviral drug baloxavir marboxil is described. The process includes a novel preparation of 2-(2,2-dimethoxyethoxy) ethanamine 13 with more convenient and safer manipulation, and a method to convert the mother liquor of the chemical resolution to the racemate 7-(benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione 6-rac. This new process has been successfully demonstrated on the 50 g scale of 13 with 66.4 % yield in 3 steps, and 10 g scale of 6-R via 9 steps with 99.9 % purity, >99 % ee and 11.0 % overall yield. All the steps just involve simple purifications without chromatography. |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000834119700001 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/302025]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Guo, Bin |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 2.Univ Sci & Technol China, Nano Sci & Technol Inst, 166 Renai Rd, Suzhou 215123, Peoples R China |
| 推荐引用方式 GB/T 7714 | Hu, Zhenfei,Li, Maocheng,Meng, Xin,et al. Improved Synthesis of Key Intermediate of Baloxavir Marboxil, an Anti-Influenza Drug[J]. CHEMISTRYSELECT,2022,7(29):5. |
| APA | Hu, Zhenfei,Li, Maocheng,Meng, Xin,&Guo, Bin.(2022).Improved Synthesis of Key Intermediate of Baloxavir Marboxil, an Anti-Influenza Drug.CHEMISTRYSELECT,7(29),5. |
| MLA | Hu, Zhenfei,et al."Improved Synthesis of Key Intermediate of Baloxavir Marboxil, an Anti-Influenza Drug".CHEMISTRYSELECT 7.29(2022):5. |
入库方式： OAI收割
来源：上海药物研究所
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