发明名称 PROCESS FOR PREPARATION OF N-(BICYCLIC HETEROCYCLYL)-4-PIPERIDINAMINES
摘要 Prepn. of piperidineamine derivs. of formula(I) and their stereoisomers and acid addn. salts comprise alkylating piperidine (III) with (II) in the presence of an inert solvent. In the formula R is H or lower alkyl; R1 is H, alkyl or Ar1 substd. lower alkyl; R2 is H, lower alkyl, (lower alkyl)-CO or Ar2-lower alkyl; L is IV, Het- Cs H2s-Y-Alk or Het-CsH2s-Z-C=X-Y-Alk; n is O or 1-2; s is O or 1-6; Alk is lower alkanediyl; Y is O,S,NR3 or directr bond; X is O, S, CH- NO2 or NR4; Z is O,S,NR5; Het is N contained 6-membered hetero ring; R3 is H or alkyl; R6 is H, alkyl or Ar2; R4 is H, alkyl, Ar2- sulphonyl, nitro or cyano; R5 is H or lower alkyl; Ar1 is halo, hydroxy or alkyl; Ar2 is halo, cyano, carboxyl or (lower alkyl)-CO-.
申请公布号 KR870001510(B1) 申请公布日期 1987.08.20
申请号 KR19830002882 申请日期 1983.06.27
申请人 JANSSEN PHARM. N.V. 发明人 JANSSEN, FRANS E.;OFFENWERT, THEOPHILUS VAN;TORREMANS, JOSEPH L.G.;HENS, JOZEF F.
分类号 C07D487/04;A61K31/416;A61K31/4162;A61K31/4523;A61P37/08;C07D211/58;C07D213/61;C07D213/74;C07D307/52;C07D401/12;C07D401/14;C07D405/14;C07D409/12;C07D409/14;C07D417/14;C07D471/04;(IPC1-7):C07D487/04 主分类号 C07D487/04
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