Process for preparing 4-chloro-3-hydroxybutanoic acid ester
    3.
    发明申请
    Process for preparing 4-chloro-3-hydroxybutanoic acid ester 审中-公开
    制备4-氯-3-羟基丁酸酯的方法

    公开(公告)号:US20060264652A1

    公开(公告)日:2006-11-23

    申请号:US10553170

    申请日:2004-04-14

    IPC分类号: C07C253/02

    摘要: The present invention relates to a process for preparing 4-chloro-3-hydroxybutanoic acid ester, an intermediate for preparing atorvastatin, in high purity and yield, by comprising the steps of 1) reacting epichlorohydrin of formula (2) with cyanide of formula (3) under the condition of pH ranging from 7 to 8, to form the 4-chloro-3-hydroxybutyronitrile of formula (4) and 2a) dissolving the 4-chloro-3-hydroxybutyronitrile of formula (4) in an alcoholic solvent and reacting it with hydrogen chloride, or 2b) reacting the 4-chloro-3-hydroxybutyronitrile of formula (4) in an alcoholic solvent saturated with hydrogen chloride, to form the 4-chloro-3-hydroxybutyronitrile acid ester of formula (I).

    摘要翻译: 本发明涉及一种制备4-氯-3-羟基丁酸酯的方法,该方法是高纯度和收率的阿托伐他汀制备中间体,包括以下步骤:1)使式(2)的表氯醇与式(2)的氰化物反应, 3)在pH为7至8的条件下,形成式(4)的4-氯-3-羟基丁腈和2a)将式(4)的4-氯-3-羟基丁腈溶解在醇溶剂中, 使其与氯化氢反应,或2b)使式(4)的4-氯-3-羟基丁腈在饱和氯化氢的醇溶剂中反应,形成式(I)的4-氯-3-羟基丁腈酸酯。