【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%。更多还原

【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.Thequinolinone amine derivative was obtained by the etherification with hydroxyquinolinone and Gabriel reaction.Thequinolinone 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%.更多还原