发明名称 PIPERAZINE DERIVATIVE AND ITS ACID ADDUCT
摘要 NEW MATERIAL:A compound of formula I [R<1> is OR<3>, NR<3>R<4> (R<3>, R<4> are H, 1-3C alkyl); R<2> is H, 1-3C alkyl; X is -C(=O)-; Ar is pyridyl, phenyl which may be substituted with halogen or 1-3C alkyl; n is 3, 4, 5] and its acid adduct. EXAMPLE:5-[5-(4-Phenyl-1-piperazinyl)valeryl]salicylamide. USE:Hypotensor: it develops satisfactory hypotensive effect with a small amount of administration, further its development is prompt and durative. Further, its high safety is suggested. PREPARATION:The reaction of an omega-halogenoalkanoylbenzene of formula II (X is halogen) with a piperazine of formula III gives the compound of formula I . The stoichiometric relation between the two reactants is 1:1, but the use of excessive amount of piperazine helps the smooth progress of the reaction and so the piperazine is used by 1-10mol per mol of the compound of formula II.
申请公布号 JPS60193978(A) 申请公布日期 1985.10.02
申请号 JP19840047965 申请日期 1984.03.13
申请人 MITSUBISHI KASEI KOGYO KK 发明人 FUKAMI JIICHI;INOUE SHINYA;NITSUTA KAZUMASA;NAKAO KENICHIROU;KIKUMOTO RIYOUJI
分类号 C07D295/08;A61K31/495;A61K31/625;A61P9/12;C07D213/74;C07D295/10 主分类号 C07D295/08
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