207238-21-9Relevant articles and documents
Practical application of the palladium-catalyzed amination in phenylpiperazine synthesis: An efficient synthesis of a metabolite of the antipsychotic agent aripiprazole
Morita, Seiji,Kitano, Kazuyoshi,Matsubara, Jun,Ohtani, Tadaaki,Kawano, Yoshikazu,Otsubo, Kenji,Uchida, Minoru
, p. 4811 - 4818 (1998)
A metabolite of Aripiprazole (1), 7-[4-[4-(2,3-dichloro-4- hydroxyphenyl)-1-piperaziyl]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 efficiently prepared using the palladium-catalyzed amination of phenyl bromide 15 with piperazine.