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    Process for the preparation of functionalised benzocyclobutenes, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
    46.
    发明申请
    Process for the preparation of functionalised benzocyclobutenes, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 失效
    用于制备官能化苯并环丁烯的方法，以及在药物可接受的酸合成伊伐布拉德及其加成盐中的应用

    公开(公告)号：US20100016580A1

    公开(公告)日：2010-01-21

    申请号：US12460208

    申请日：2009-07-15

    申请人： Jean-Louis Peglion ,  Olivier Baudoin ,  Nicolas Audic ,  Manon Chaumontet ,  Riccardo Piccardi

    发明人： Jean-Louis Peglion ,  Olivier Baudoin ,  Nicolas Audic ,  Manon Chaumontet ,  Riccardo Piccardi

    IPC分类号： C07D223/16 ,  C07C41/01

    CPC分类号： C07C51/38 ,  C07B37/10 ,  C07B2200/07 ,  C07C62/34 ,  C07C67/317 ,  C07C67/32 ,  C07C69/753 ,  C07C69/757 ,  C07C253/30 ,  C07C2602/22 ,  C07D223/16 ,  C07F7/1804 ,  C07C69/76 ,  C07C255/47

    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.

    摘要翻译： 制备式（IV）化合物的方法：其中可以相同或不同的R 1，R 2，R 3和R 4各自表示氢原子，直链或支链（C 1 -C 6）烷基，直链或支链 （C1-C6）烷氧基，氟原子，氯原子，被保护的胺基，保护的羟基，烷氧基为直链或支链的烷氧基羰基（C1-C6）或CF3基，或 R1-R4-H和R2和R3与携带它们的碳原子一起形成1,3-二氧戊环基团，R 5表示饱和或不饱和的直链或支链（C 1 -C 6）烷基，直链或支链（C1- C6）羟基官能团的羟烷基或其中R 7为直链或支链（C 1 -C 6）烷基的CO 2 R 7基团，R 6表示其中R 8为直链或支链的氰基或CO 2 R 8基团（ C1-C6） - 烷基。 在伊伐溴丁的合成中的应用，其与药学上可接受的酸及其水合物的加成盐。