Improved Synthesis of 6-Chloro-5-methylpyridin-2-amine: A Key Intermediate for Making Lumacaftor
文献类型：期刊论文
| 作者 | Zhang, Junchi1,2; Zhu, Fuqiang3; Tian, Guanghui3; Jiang, Xiangrui1,2 ; Shen, Jingshan1,2
|
| 刊名 | ORGANIC PROCESS RESEARCH & DEVELOPMENT
 |
| 出版日期 | 2020-06-19 |
| 卷号 | 24期号:6页码:1175-1179 |
| 关键词 | 6-chloro-5-methylpyridin-2-amine lumacaftor methylation safe |
| ISSN号 | 1083-6160 |
| DOI | 10.1021/acs.oprd.9b00556 |
| 通讯作者 | Jiang, Xiangrui(jiangxiangrui@simm.ac.cn) |
| 英文摘要 | A safe and efficient synthesis of 6-chloro-5-methylpyridin-2-amine, a key intermediate for lumacaftor, is described, which avoids the utilization of peroxide. In this four-step sequence, starting from 2-amino-6-chloropyridine, the crucial 5-position methylation was achieved via a Suzuki-Miyaura cross-coupling reaction. By adopting this synthetic route, 6-chloro-5-methylpyridin-2-amine was produced on a hectogram scale with 62.4% overall yield and 99.49% purity. |
| WOS关键词 | CYSTIC-FIBROSIS PATIENTS |
| 资助项目 | Special Foundation of the Chinese Academy of Sciences for strategic pilot technology[XDA12050411] ; Special Foundation of the Chinese Academy of Sciences for strategic pilot technology[XDA12040327] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000543672300028 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/291752]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Jiang, Xiangrui |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 3.Topharman Shanghai Co Ltd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Junchi,Zhu, Fuqiang,Tian, Guanghui,et al. Improved Synthesis of 6-Chloro-5-methylpyridin-2-amine: A Key Intermediate for Making Lumacaftor[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2020,24(6):1175-1179. |
| APA | Zhang, Junchi,Zhu, Fuqiang,Tian, Guanghui,Jiang, Xiangrui,&Shen, Jingshan.(2020).Improved Synthesis of 6-Chloro-5-methylpyridin-2-amine: A Key Intermediate for Making Lumacaftor.ORGANIC PROCESS RESEARCH & DEVELOPMENT,24(6),1175-1179. |
| MLA | Zhang, Junchi,et al."Improved Synthesis of 6-Chloro-5-methylpyridin-2-amine: A Key Intermediate for Making Lumacaftor".ORGANIC PROCESS RESEARCH & DEVELOPMENT 24.6(2020):1175-1179. |
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。