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METHOD FOR PREPARATION OF PERINDOPRIL WITH USAGE OF TETRAMETHYL-URONIUM SALTS AS REAGENT OF COUPLING REACTION
METHOD FOR PREPARATION OF PERINDOPRIL WITH USAGE OF TETRAMETHYL-URONIUM SALTS AS REAGENT OF COUPLING REACTION
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机译:以四甲基-铀盐为偶联反应试剂制备培哚普利的方法
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摘要
FIELD: chemistry.;SUBSTANCE: invention refers to the selective method for preparation of "АХЭ" inhibitor - perindopril with usage as initial reagent of the sterospecific amino acid N-/1-(S)-ethoxycarbonylbutyl/-(S)-alanine which is activated by tetramethyl-uronium salts in the presence of tertiary organic base and following interreaction with (2S,3aS,7aS)-octahydroindolo-2-carbonic acid or its ester. After completing of the reaction the protective group is removed by the hydrogenation, interphase hydrogenation or extraction.;EFFECT: obtaining of perindopril with usage of tetramethyl-uronium salts as reagents of coupling reaction.;5 cl, 3 ex
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机译:发明领域:本发明涉及选择性地制备“АХЭ”抑制剂-培哚普利的方法,该试剂用作立体特异性氨基酸N- / 1-(S)-乙氧基羰基丁基/-(S)-丙氨酸的起始试剂,在叔有机碱存在下并与(2S,3aS,7aS)-八氢吲哚-2-碳酸或其酯相互作用后,四甲基铀盐将其活化。反应完成后,通过氢化,相间氢化或萃取除去保护基。效果:使用四甲基铀盐作为偶联反应试剂获得培哚普利; 5 cl,3 ex
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