发明名称 PROCESS FOR THE SYSTHESIS OF 7,8-DIMETHOXY-1,3-DIHYDRO-2H-3-BENZAZEPIN-2-ONE COMPOUNDS AND APPLICATION IN THE SYNTHESIS OF IVABRADINE
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.
申请公布号 ZA201402072(B) 申请公布日期 2015.03.25
申请号 ZA20140002072 申请日期 2014.03.20
申请人 LES LABORATOIRES SERVIER 发明人 LE FLOHIC,ALEXANDRE
分类号 C07D;C07F 主分类号 C07D
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