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METHOD FOR ENANTIOSELECTIVE SYNTHESIS OF (S)-PREGABALIN

机译:对映体合成(S)-培拉巴林的方法

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to a method of producing (S)-pregabalin of formula I , which is used in therapy of a range of neuropathic diseases. The method includes enantioselective addition of diethyl malonate to 4-methyl-1-nitropentene-1 followed by reduction and acid hydrolysis of the addition product in accordance with the given scheme. The catalyst used at the addition step is a complex of nickel (II) of formula II with (S,S)-N,N'-dibenzylcyclohexane-1,2-diamine.;EFFECT: method reduces catalyst consumption, reduces the number of steps and amount of solvents used, thereby making the process simpler and cheaper.;4 cl, 10 ex
机译:技术领域本发明涉及一种制备式I的(S)-普瑞巴林的方法。<图像文件=“ 00000008.GIF” he =“ 56” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 153 “ />,用于治疗多种神经性疾病。该方法包括根据给定方案将丙二酸二乙酯对映选择性加成到4-甲基-1-硝基戊烯-1中,然后还原和酸水解加成产物。在加成步骤中使用的催化剂是式II的镍(II)的配合物 <图片文件=“ 00000009.GIF” he =“ 35” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 56” />与(S,S)-N,N'-二苄基环己烷-1,2-二胺。效果:该方法减少了催化剂的消耗,减少了步骤数并减少了溶剂用量,从而使该方法更简单,更便宜。; 4 cl,10 ex

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