A New and Improved Process for N-(4-Chloro-3-cyano-7-ethoxyquinolin-6-yl)acetamide
文献类型：期刊论文
| 作者 | Mao, Yongjun2; Liu, Zheng1; Yang, Xiaojun1; Xia, Xiangfei1; Zhang, Rongxia2 ; Li, Jianfeng2; Jiang, Xiangrui2; Xie, Kai1; Zheng, Jin1; Zhang, Hui1
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| 刊名 | ORGANIC PROCESS RESEARCH & DEVELOPMENT
 |
| 出版日期 | 2012-12 |
| 卷号 | 16期号:12页码:1970-1973 |
| ISSN号 | 1083-6160 |
| DOI | 10.1021/op300260m |
| 文献子类 | Article |
| 英文摘要 | A new and improved synthetic route to N-(4-chloro-3-cyano-7-ethoxyquinolin-6-yl)acetamide (1) is described on a kilogram scale. The key step is the basic cyclization of o-[(2-cyanovinyl)amino]benzoate (14) in (BuONa)-Bu-t/(BuOH)-Bu-t system to give the 3-cyano-4-hydroxyquinoline (7). The final product 1 is obtained with 49% overall yield (seven steps) and 98.9% purity (HPLC), which makes it a cost-effective and commercially friendly process for scale-up operations. |
| WOS关键词 | KINASE-ACTIVITY ; INHIBITORS ; OPTIMIZATION ; ENAMINONES ; DISCOVERY ; AGENTS ; HER-2 ; EGFR |
| 资助项目 | National Science and Technology Major Project[2012ZX09301001-001] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000313147900012 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277858]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Shen, Jingshan |
| 作者单位 | 1.Topharman Shanghai Co Ltd, Shanghai 201209, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Mao, Yongjun,Liu, Zheng,Yang, Xiaojun,et al. A New and Improved Process for N-(4-Chloro-3-cyano-7-ethoxyquinolin-6-yl)acetamide[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2012,16(12):1970-1973. |
| APA | Mao, Yongjun.,Liu, Zheng.,Yang, Xiaojun.,Xia, Xiangfei.,Zhang, Rongxia.,...&Shen, Jingshan.(2012).A New and Improved Process for N-(4-Chloro-3-cyano-7-ethoxyquinolin-6-yl)acetamide.ORGANIC PROCESS RESEARCH & DEVELOPMENT,16(12),1970-1973. |
| MLA | Mao, Yongjun,et al."A New and Improved Process for N-(4-Chloro-3-cyano-7-ethoxyquinolin-6-yl)acetamide".ORGANIC PROCESS RESEARCH & DEVELOPMENT 16.12(2012):1970-1973. |
入库方式： OAI收割
来源：上海药物研究所
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