Preparation of 7-[4-(Piperazine-1-yl)butoxy]quinoline-2-(1H)-ketone
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％.
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