New and Practical Synthesis of N-(3-Cyano-7-ethoxy-4-oxo-1, 4-dihydroquinolin-6-yl)acetamide

被引:1
|
作者
Ma, Wenpeng [1 ]
Mao, Yongjun [2 ]
Xie, Kai [3 ]
Zhu, Qifeng [3 ]
Zhang, Rongxia [2 ]
Shen, Jingshan [2 ]
Sun, Hongbin [1 ]
机构
[1] China Pharmaceut Univ, Nanjing 210009, Jiangsu, Peoples R China
[2] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
[3] Topharman Shanghai Co Ltd, Shanghai 201209, Peoples R China
关键词
ADDITION-ELIMINATION REACTION; KINASE-ACTIVITY; INHIBITORS; OPTIMIZATION; DERIVATIVES; DISCOVERY; SUBSTRATE; AGENTS; HER-2; EGFR;
D O I
10.1002/jhet.1901
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
New and practical synthetic route of N-(3-cyano-7-ethoxy-4-oxo-1,4-dihydroquinolin-6-yl)acetamide (1) is described, through the cyclization of 2-aminophenyl-ethanone (12) with N,N-dimethylformamide dimethylacetal. The overall yield of 1 obtained from this process is 46% (five steps) with a purity of >99% (HPLC).
引用
收藏
页码:866 / 868
页数:3
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