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3-phenyl-3-(substd-amino)-3,4-dihydro-isocoumarins - and isochromans - as anti hypertensive agents and diuretics

机译:3-苯基-3-(取代氨基)-3,4-二氢-异香豆素-和异色满-作为抗高血压药和利尿剂

摘要

Cpds. of the formula: (where R is H, CF3 or 1-5C-alkyl or -alkoxy, R1 is H, F, Cl, CF3 1-5C-alkyl or -alkoxy or two R1 together form -O-CH2-O-, R2 is H, F, Cl, CF3 or 1-5C-alkoxy, R3 and R4 are 1-5C alkyl, 2-5C alkenyl or PhCH2 or NR3R4 is 1-pyrrolidinyl, piperidino, 1-azepinyl 1-azocinyl, morpholino, thiomorpholino, or 4-(1-5C)-alkyl-1-piperazinyl, R5 is H or 1-5C alkyl, X is CH2 or CO, at most three of R,R1 and R2 are other than H and two of R, R1 and R2 are h on each ring, R and R2 are not both halogen and two CF3 gps. may not be present on adjacent C-atoms) are prepared by reacting an o-methyl-N-alkylbenzamide Li salt with a di-substd amino propiophenone and ring closing the o- beta-(2.di substd aminoethyl)-beta-hydroxy-phenethyl-N-alkylbenzamide by heating at 100 degrees C.
机译:Cpds。式(其中R是H,CF 3或1-5C-烷基或-烷氧基,R 1是H,F,Cl,CF 3 1-5C-烷基或-烷氧基或两个R 1一起形成-O-CH 2 -O- ,R 2是H,F,Cl,CF 3或1-5 C-烷氧基,R 3和R 4是1-5 C烷基,2-5 C烯基或PhCH 2或NR 3 R 4是1-吡咯烷基,哌啶子基,1-a庚基1-偶氮基,吗啉代,硫吗啉代或4-(1-5C)-烷基-1-哌嗪基,R5为H或1-5C烷基,X为CH2或CO,R,R1和R2中的至多三个不为H,两个为R, R1和R2在每个环上均为h,R和R2都不都是卤素,并且两个CF3 gps(可能不存在于相邻的C原子上)是通过使邻甲基-N-烷基苯甲酰胺Li盐与二取代基反应制得的氨基苯乙酮并通过在大于100摄氏度的温度下加热使o-β-(2.di取代氨基乙基)-β-羟基-苯乙基-N-烷基苯甲酰胺闭环

著录项

  • 公开/公告号FR2178718A1

    专利类型

  • 公开/公告日1973-11-16

    原文格式PDF

  • 申请/专利权人 SANDOZ SAFR;

    申请/专利号FR19720011734

  • 发明设计人

    申请日1972-04-04

  • 分类号A61K27/00;C07D7/00;

  • 国家 FR

  • 入库时间 2022-08-23 05:16:07

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