PROCESS FOR THE PREPARATION OF ASPARTYL PEPTIDES AND NEW SYNTHETIC INTERMEDIATES

摘要

THE INVENTION RELATES TO THE PREPARATION OF ASPARTYL PEPTIDES OF GENERAL FORMULA IV: BR/ (CF DRAWING IN BOPI) BR/ IN WHICH -NHR REPRESENTS A REMAINDER OF AMINO ACID OR PEPTIDE. FOLLOWING THE INVENTION, A B-MONOESTER OF ASPARTIC ACID OF GENERAL FORMULA1: BR/ (CF DRAWING IN BOPI) BR/ IN WHICH R REPRESENTS A HYDROCARBON RADICAL POSSIBLY CARRYING AN ACTIVATOR SUBSTITUTE, WITH A COMPOUND B-DICARBONYL, SUCH AS ETHYL ACETYL ACETATE, TO FORM AN ENAMINE ON WHICH COUPLING WITH AN AMINO ACID OR A DERIVATIVE SUCH AS AN ESTER OR A PEPTIDE, PREVIOUSLY PROTECTED IF NECESSARY, AND ELIMINATED IF NECESSARY, PROTECTIVE GROUPS. /P P THE PROCESS MAKES IT POSSIBLE TO OBTAIN A-ASPARTYL PEPTIDES EXEMPTED FROM ISOMEREB.