Tetrahedron

Practical application of the palladium-catalyzed amination in phenylpiperazine synthesis: an efficient synthesis of a metabolite of the antipsychotic agent aripiprazole

…, K Kitano, J Matsubara, T Ohtani, Y Kawano, K Otsubo…

文献索引：Morita, Seiji; Kitano, Kazuyoshi; Matsubara, Jun; Ohtani, Tadaaki; Kawano, Yoshikazu; Otsubo, Kenji; Uchida, Minoru Tetrahedron, 1998 , vol. 54, # 19 p. 4811 - 4818

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被引用次数: 53

摘要

A metabolite of Aripiprazole (1), 7-[4-[4-(2, 3-dichloro-4-hydroxyphenyl)-1-piperazinyl] butoxy]-3, 4-dihydro-2 (1H)-quinolinone (2), was prepared by the coupling reaction of 1-(4- benzyloxy-2, 3-dichlorophenyl)-piperazine (11) with 7-(4-chlorobutoxy)-3, 4-dihydro-2 (1H)- quinolinone (16). The palladium-catalyzed amination of contiguous tri-and tetra-substituted benzenes with piperazine derivatives was investigated. The key intermediate 11 was ...