Invention Grant
- Patent Title: Process for the preparation of functionalised benzocyclobutenes, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
- Patent Title (中): 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
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Application No.: US12460208Application Date: 2009-07-15
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Publication No.: US08110701B2Publication Date: 2012-02-07
- Inventor: Jean-Louis Peglion , Olivier Baudoin , Nicolas Audic , Manon Chaumontet , Riccardo Piccardi
- Applicant: Jean-Louis Peglion , Olivier Baudoin , Nicolas Audic , Manon Chaumontet , Riccardo Piccardi
- Applicant Address: FR Suresnes Cedex FR Paris Cedex FR Villeurbanne Cedex
- Assignee: Les Laboratoires Servier,Centre National de la Recherche Scientifique,Universite Claude Bernard Lyon 1
- Current Assignee: Les Laboratoires Servier,Centre National de la Recherche Scientifique,Universite Claude Bernard Lyon 1
- Current Assignee Address: FR Suresnes Cedex FR Paris Cedex FR Villeurbanne Cedex
- Agency: Hueschen and Sage
- Priority: FR0804061 20080717
- Main IPC: C07C69/76
- IPC: C07C69/76

Abstract:
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.
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