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PROCESS FOR THE INDUSTRIAL SYNTHESIS OF (2S, 3AS, 7AS) 2-CARBOXY PERHYDROINDOLE. APPLICATION TO THE INDUSTRIAL SYNTHESIS OF CARBOXYALKYL DIPEPTIDES
PROCESS FOR THE INDUSTRIAL SYNTHESIS OF (2S, 3AS, 7AS) 2-CARBOXY PERHYDROINDOLE. APPLICATION TO THE INDUSTRIAL SYNTHESIS OF CARBOXYALKYL DIPEPTIDES
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机译:工业合成(2S,3AS,7AS)2-羧基全吲哚的过程。在羧二肽工业合成中的应用
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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. Application to the synthesis of carboxyalkyl d peptides capable of being employed in therapeutics.
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