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Process for the industrial synthesis of (2S, 3aS, 7aS) 2-carboxy perhydroindole, application to the industrial synthesis of carboxyalkyl dipeptides

机译:(2S,3aS,7aS)2-羧基全氢吲哚的工业合成方法,应用于羧烷基二肽的工业合成

摘要

Process for the industrial synthesis of (2S, 3 7aS)-2- carboxyperhydroindole by reduction of 2-carbox indole or of one of its esters to (R,S)-2-carboxyindo or of one of its esters which, after saponification, converted into the acid, the S isomer cf (R,S)-2- carboxyindoline being obtained by precipitation from the mixture of the two (R) and (S) isomers, in the presence of (+) methylbenzylamine, (S)-2- carboxyindoline being in its turn subjected to catalytic hydrogenation to give (2S, 3aS,7aS)-2-carboxyperhydroindole, after separation of (2S,3aR, 7aR) isomer by crystallization.PPApplication to the synthesis of carboxyalkyl d peptides capable of being employed in therapeutics.
机译:工业合成(2S,3 7aS)-2-羧基过氢吲哚的方法,是将2-羧基吲哚或其酯中的一种还原为(R,S)-2-羧基吲哚或其酯中的一种,然后将其皂化,在(+)甲基苄胺,(S)-存在下,通过从两种(R)和(S)异构体的混合物中沉淀获得S异构体cf(R,S)-2-羧基二氢吲哚。通过结晶分离(2S,3aR,7aR)异构体后,将2-羧基二氢吲哚依次进行催化氢化得到(2S,3aS,7aS)-2-羧基全氢吲哚。能够用于治疗的羧烷基D肽。

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