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2,2'-DISUBSTITUTED-ETHANESULFONIC ACID DERIVATIVE AND ITS SALT

机译:2,2'-取代的乙磺酸衍生物及其盐

摘要

PROBLEM TO BE SOLVED: To obtain a new ethanesulfonic acid derivative or its salt useful as an optical resolution agent, pharmaceuticals such as antiarrhythmic agent or an agent for the treatment of arteriosclerosis, etc., its intermediate, a raw material for agrochemicals, etc. ;SOLUTION: The objective compound is an ethanesulfonic acid derivative of formula I (R1 is H or a 1-8C alkyl; R2 is a 1-8C alkyl; * represents the position of an asymmetric carbon atom) or its salt, e.g. (s)-2-p- isobutylphenylpropanesulfonic acid. The compound of formula I can be produced by reacting a halogenated ethyl derivative of formula II (X is a halogen) with an alkali metal sulfite in a proper solvent to obtain an alkali metal salt of an ethanesulfonic acid derivative and optionally converting the alkali metal salt into sulfonic acid by using an ion exchange resin or by double decomposition. Optical resolution of an amine compound of formula III (R3 is an aryl, an alkyl or an alkoxy; R4 is an alkyl; A is CH2, etc.) can be performed by using the compound of formula I as an optical resolution agent.;COPYRIGHT: (C)1997,JPO
机译:解决的问题:为了获得新的乙磺酸衍生物或其盐作为旋光拆分剂,抗心律不齐药物或动脉硬化治疗剂等药物,其中间体,农用化学品的原料等。 ;解决方案:目标化合物为式I的乙磺酸衍生物(R 1 为H或1-8C烷基; R 2 为1-8C烷基; *代表不对称碳原子或其盐的位置,例如(s)-2-对-异丁基苯基丙烷磺酸。式I的化合物可以通过在适当的溶剂中使式II的卤代乙基衍生物(X为卤素)与碱金属亚硫酸盐反应以获得乙磺酸衍生物的碱金属盐并任选地将碱金属盐转化而制备。通过使用离子交换树脂或通过双重分解生成磺酸。式III(R 3 为芳基,烷基或烷氧基; R 4 为烷基; A为CH 2 < / Sub>等)可以通过使用式I的化合物作为光学拆分剂来进行。;版权:(C)1997,JPO

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