发明名称 PROCESS FOR PREPARING 1-(CYCCOHEXYL)-4-ARYL-4-PIPERIDINE CARBOXYLIC ACID DERIVATIVES
摘要 Cyclohexylpiperidines I (R = OH, esterified OH, amino; R1 = H, alkyl; Ar1, Ar2 = optionally substituted Ph, thienyl, pyridyl) were prepared. Thus, 4-oxo-1-(2-piridinyl)cyclohexanecarbonitrile was treated with Et 4-phenyl-4-piperidinecarboxylate, followed by redn., to give I (R = OEt, R1 = H, Ar1 = 2-pyridinyl, Ar2 = phenyl). I have antihistaminic acitivity. Thus, I (R = OEt, R1 = H, Ar1 = 4-FC6H4, Ar2 = phenyl) protected rats against the lethal effects of compounds 48/80 at 0.04 mg/kg orally.
申请公布号 KR840002003(B1) 申请公布日期 1984.10.27
申请号 KR19840004375 申请日期 1984.07.24
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 STOKBROEKX, RAYMOND A.;LUYCKX, MARCEL G.M.;WILLEMS, JOANNES J.M.
分类号 C07D211/64;A61K;A61K31/445;A61K31/451;A61P37/08;C07C25/13;C07C33/46;C07D;C07D211/96;C07D213/57;C07D401/08;(IPC1-7):C07D211/64 主分类号 C07D211/64
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