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

作　　者：刘丹 彭子祥 刘进兵 LIU Dan;PENG Zixiang;LIU Jinbing(School of Food and Chemical Engineering,Shaoyang University,Shaoyang 422099)

机构地区：[1]邵阳学院食品与化学工程学院,湖南邵阳422099

出　　处：《中国医药工业杂志》2024年第6期800-803,共4页Chinese Journal of Pharmaceuticals

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%。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 HCI/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 

分 类 号：TQ460.6[化学工程—制药化工] R971.43[医药卫生—药品]