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process for the preparation of l (-) - carnitine chloride from 3.4 - epossibutirrici foreign

机译:3.4制备l(-)-氯化肉碱的方法-epossibutirrici Foreign

摘要

Disclosed is a process for the preparation of the L(-)-carnitine chloride having formula (I): …CHEM… which comprises:… a) reacting a racemic ester of (R, S)-3, 4-epoxybutyric acid having formula (II): …CHEM… wherein R represents a C1-C10 alkyl group or a benzyl group, with an enzyme or with a microorganism producing said enzyme, capable of hydrolyzing asymmetrically and in a prevalent way, enanitiomer S(-), and separating said enantiomer S(-) according to usual techniques from non-reacted ester (III) which is substantially present in the R(+) form;… b) reacting said ester (II) in its form R(+) or the corresponding chlorohydrin having formula (III), obtained by reaction with hydrochloric acid or with a chlorotrialkylsilane, …CHEM… with trimenthylamine hydrochloride or with trimethylamine itself, respectively, to obtain an ester having formula (IV): …CHEM… and… c) hydrolyzing said ester having formula (IV) in the presence of HCL to obtain L(-)-carnitine chloride having formula (I).… L(-)-carnitine is an eutrophic and cardioprotecting agent for the cure of myocardic ischemia, angina pectoris and myocardium sclerosis.… The R(+) forms of the esters of 3, 4-epoxybutyric acid, obtained in step (a) of the process are intermediate products.
机译:公开了一种具有式(I)的L(-)-肉碱氯化物的制备方法:……,其包括:…a)使(R,S)-3,4-环氧丁酸的外消旋酯反应具有式(II)的化合物:...其中R代表C 1 -C 10烷基或苄基,其中所述酶或微生物与产生所述酶的微生物能够以不对称且普遍的方式水解对映体S(- ),并根据常规技术从基本上以R(+)形式存在的未反应的酯(III)中分离出所述对映体S(-);…b)以R(+)形式使所述酯(II)反应或分别通过与盐酸或三氯氯代烷基硅烷,……与三薄荷胺盐酸盐或与三甲胺本身反应而获得的具有式(III)的氯代醇,从而获得具有式(IV)的酯:… …和…c)在HCl存在下水解所述具有式(IV)的酯以获得具有式(I)的L(-)-肉碱氯化物).... L(-)-肉碱是一种富营养性和心脏保护剂,可用于治疗心肌缺血,心绞痛和心肌硬化。…R(+)形式的3,4-环氧丁酸酯,在步骤( a)该过程是中间产品。

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