发明名称 Method for the production of 5-(4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl-benzofuran-2-carboxamide
摘要 Preparation of 5-(4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (A) and/or their salts comprises either reacting a heterocyclic compound (I) with 3-(4-piperazine-1-yl-butyl)-indol-5-carbonitrile by transition metal catalyzed coupler using palladium complex; and /or converting the obtained (A) to its acid addition salt by treating with an acid; or reacting a heterocyclic compound (II) with 3-(4-oxo-butyl)-1H-indol-5-carbonitrile by reductive amination; and/or converting the obtained (A) to an acid addition salt by treating with an acid. Preparation of 5-(4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (A) and/or their salts comprises either reacting a heterocyclic compound of formula (I) with 3-(4-piperazine-1-yl-butyl)-indol-5-carbonitrile by transition metal catalyzed coupler using palladium complex; and/or converting the obtained (A) to its acid addition salt by treating with an acid; or reacting a heterocyclic compound of formula (II) (as a base or HX salt) with 3-(4-oxo-butyl)-1H-indol-5-carbonitrile by reductive amination; and/or converting the obtained (A) to an acid addition salt by treating with an acid. L : Cl, Br, I, SO 2F, SO 2CF 3, SO 2C 2F 5; and X : Cl or Br. [Image].
申请公布号 ZA200710145(B) 申请公布日期 2008.11.26
申请号 ZA20070010145 申请日期 2007.11.26
申请人 MERCK PATENT GMBH 发明人 BATHE, ANDREAS
分类号 C07D 主分类号 C07D
代理机构 代理人
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