发明名称 Process for the enzymatic synthesis of (7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-triene-7-carboxylic acid or esters thereof, and application in the synthesis of ivabradine and salts thereof
摘要 The present invention relates to a process for the enzymatic synthesis of the compound of formula (I):wherein R1 represents a hydrogen atom or a C1-C6 alkyl group, preferably methyl, and also to its application in the synthesis of ivabradine of formula (II):or 3-{3-[{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino]propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one, its addition salts with a pharmaceutically acceptable acid and their hydrates.The use of hydrolytic enzymes (hydrolases), which function without cofactors, such as lipases or esterases, makes it possible to obtain chiral compounds - key intermediates in the synthesis of pharmaceutical active ingredients - in high enantiomeric excesses and good yields.
申请公布号 MD20130008(A2) 申请公布日期 2013.07.31
申请号 MD20130000008 申请日期 2013.02.07
申请人 LES LABORATOIRES SERVIER 发明人 PEDRAGOSA MOREAU SANDRINE;LEFOULON FRANCOIS;LEFOULON FRANCOIS
分类号 C07C13/44;C07B53/00;C07B57/00;C07C39/14;C07C39/17;C07C43/275;C07C209/26;C07C211/11;C07C217/56;C07D223/16;C12N9/18;C12N9/20 主分类号 C07C13/44
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