首页> 外国专利> PROCESS FOR THE SYNTHESIS OF 7,8-DIMETHOXY-1,3-DIHYDRO-2H-3-BENZAZEPIN-2-ONE COMPOUNDS, AND APPLICATION IN THE SYNTHESIS OF IVABRADINE

PROCESS FOR THE SYNTHESIS OF 7,8-DIMETHOXY-1,3-DIHYDRO-2H-3-BENZAZEPIN-2-ONE COMPOUNDS, AND APPLICATION IN THE SYNTHESIS OF IVABRADINE

机译:7,8-二甲氧基-1,3-二氢-2H-3-苯并二氮杂-2-酮化合物的合成方法及其在合成艾达巴定中的应用

摘要

Synthesis of dihydro-1H-benzo[d]azepine (I) involves subjecting 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepine-2,4-dione (VII) to reduction reaction in presence of lithium triethylborohydride in an organic solvent. Synthesis of dihydro-1H-benzo[d]azepine of formula (I) involves subjecting 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepine-2,4-dione of formula (VII) to reduction reaction in presence of lithium triethylborohydride in an organic solvent. R : p-methoxybenzyl or group of formula (i). Independent claims are included for the following: (1) 3-[3-({[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1(6),2,4-trien-7-yl]methyl}(methyl)amino)propyl]-7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepine-2,4-dione; and (2) 2-[2-({[3-({[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1(6),2,4-trien-7-yl]methyl}(methyl)amino)propyl]carbamoyl}methyl)-4,5-dimethoxyphenyl]acetic acid. [Image] ACTIVITY : Antianginal; Antiarrhythmic; Cardiant; Vasotropic.
机译:二氢-1H-苯并[d] a庚因的合成(I)涉及使7,8-二甲氧基-2,3,4,5-四氢-1H-3-苯并ze庚因-2,4-二酮(VII)在在有机溶剂中存在三乙基硼氢化锂。式(I)的二氢-1H-苯并[d] a庚因的合成涉及使式(VII)的7,8-二甲氧基-2,3,4,5-四氢-1H-3-苯并ze庚因-2,4-二酮在有机溶剂中在三乙基硼氢化锂存在下还原反应。 R:对甲氧基苄基或式(i)的基团。包括以下方面的独立权利要求:(1)3- [3-({[((7S)-3,4-dimethoxymethoxycyclocyclo [4.2.0] octa-1(6),2,4-trien-7-yl]甲基}(甲基)氨基)丙基] -7,8-二甲氧基-2,3,4,5-四氢-1H-3-苯并ze庚因-2,4-二酮;和(2)2- [2-({[3-({[(7S)-3,4-dimethoxydicyclobicyclo [4.2.0] octa-1(6),2,4-trien-7-yl] methyl}} (甲基)氨基)丙基]氨基甲酰基}甲基)-4,5-二甲氧基苯基]乙酸。活动:抗心绞痛;抗心律不整;卡迪恩变压的。

著录项

  • 公开/公告号SG10201400610SA

    专利类型

  • 公开/公告日2014-10-30

    原文格式PDF

  • 申请/专利权人 LES LABORATOIRES SERVIER;

    申请/专利号SG10201400610S

  • 发明设计人 ALEXANDRE LE FLOHIC;

    申请日2014-03-13

  • 分类号

  • 国家 SG

  • 入库时间 2022-08-21 15:55:48

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