发明名称 1,2,4 TRIAZOL-3-ONE ANTIDEPRESSANTS AND THEIR PREPARATION
摘要 The title cpds. (I)[R=H, halog, alkoxy, CF3; R1=H, alkyl; R2=CH2Ph, (un)substd. Ph, 2-pyridyl, pyrimidyl, 2-quinolinyl, 3benzisothazoyl; x=0, bond; n=2-4 were prepd.. Thus, piperazine (II)(R3=H) was N- alkylated with Br(CH2)3Cl to give 66% (II)[R3= (CH2)3Cl , which was treated with N2H4 to give 92% (II)[R3= (CH2)3NHNH2 . The cyclocondensation of (II) with EtC(S)NHCO2Et gave 72% piperazinopropyltriazole (III)(R4=H), which was Nalkylated with PhOCH2CH2Br to give 53% (III)(R4=CH2CH2OPh)(IV). (IV) is an antidepressant with minimal potential for side effects such as sedation and blood pressure lowering.
申请公布号 KR890000637(B1) 申请公布日期 1989.03.22
申请号 KR19840003692 申请日期 1984.06.28
申请人 BRISTOL-MYERS COMPANY 发明人 TEMPLE, DAVIS L JR;LOBECK, WALTER G JR
分类号 A61K31/495;A61P25/24;A61P25/26;C07D213/74;C07D215/38;C07D241/20;C07D249/08;C07D249/12;C07D275/04;C07D295/06;C07D295/067;C07D295/13;C07D295/15;C07D401/06;C07D401/12;C07D401/14;C07D403/06;C07D403/12;C07D403/14;C07D417/12;C07D417/14;(IPC1-7):C07D401/06 主分类号 A61K31/495
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