发明名称 Process for the preparation of functionalised benzocyclobutenes, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
摘要 Process for the preparation of compounds of formula (IV): wherein R1, R2, R3 and R4, which may be identical or different, each represent a hydrogen atom, a linear or branched (C1-C6)alkyl group, a linear or branched (C1-C6)alkoxy group, a fluorine atom, a chlorine atom, a protected amine group, a protected hydroxyl group, an alkoxycarbonyl group in which the alkoxy group is linear or branched (C1-C6), or a CF3 group, or R1-R4-H and R2 and R3 together with the carbon atoms carrying them form a 1,3-dioxolane group, R5 represents a saturated or unsaturated, linear or branched (C1-C6)alkyl group, a linear or branched (C1-C6)hydroxyalkyl group in which the hydroxyl function is protected, or a CO2R7 group in which R7 is a linear or branched (C1-C6)alkyl group, R6 represents a cyano group or a CO2R8 group in which R8 is a linear or branched (C1-C6)-alkyl group. Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
申请公布号 US2010016580(A1) 申请公布日期 2010.01.21
申请号 US20090460208 申请日期 2009.07.15
申请人 LES LABORATOIRES SERVIER;CENTRE NATIONAL DE LA RECHERCHE;UNIVERSITE CLAUDE BERNARD LYON 1 发明人 PEGLION JEAN-LOUIS;BAUDOIN OLIVIER;AUDIC NICOLAS;CHAUMONTET MANON;PICCARDI RICCARDO
分类号 C07D223/16;C07C41/01 主分类号 C07D223/16
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