7-[4-(哌嗪-1-基)丁氧基]喹啉-2-(1H)-酮的制备
Preparation of 7-[4-(Piperazine-1-yl)butoxy]quinoline-2-(1H)-ketone
刘丹 1彭子祥 1刘进兵1
作者信息
- 1. 邵阳学院食品与化学工程学院,湖南邵阳 422099
- 折叠
摘要
7-[4-(哌嗪-1-基)丁氧基]喹啉-2-(1H)-酮(1)是依匹哌唑的关键中间体.该研究以1,4-二卤代丁烷为原料,先和邻苯二甲酰亚胺化合物反应,得到N-烃基化邻苯二甲酰亚胺,再和羟基喹啉酮醚化,经过Gabriel反应得到喹啉酮胺衍生物,将所得喹啉酮胺与N,N-双(2-氯乙基)氨基甲酸叔丁酯闭环得到Boc保护的1,最后用HCl/MeOH脱保护得1,总收率为22％,纯度99％.
Abstract
7-[4-(Piperazine-1-yl)butoxy]quinoline-2-(1H)-ketone(1)is a key intermediate of brexpiprazole.In this paper,N-alkylated phthalimide was obtained by the reaction of phthalimide compound with 1,4-dihalobutane.The quinolinone amine derivative was obtained by the etherification with hydroxyquinolinone and Gabriel reaction.The quinolinone amine derivative was cyclized with tert-butyl N,N-bis(2-chloroethyl)carbamate followed by deprotection of Boc with HCl/MeOH to get the target compound 1 with the overall yield of 22％and purity of 99％.
关键词
7-[4-(哌嗪-1-基)丁氧基]喹啉-2-(1H)-酮/依匹哌唑/中间体/制备Key words
7-[4-(piperazine-1-yl)butoxy]quinoline-2-(1H)-ketone/brexpiprazole/intermediate/preparation引用本文复制引用
出版年
2024
NETL
NSTL
万方数据