PROCESS FOR THE PREPARATION OF NEW DERIVATIVES OF GLUTAMIC ACID AND ASPARTIC ACID HAVING ANTAGONISTIC ACTIVITIES TOWARDS BIOACTIVE POLYPEPTIDES

摘要

or -aspartic acid derivs. of formula (I) and their salts are new. n = 1 or 2; R1 = phenyl mono-, di-or trisubstd. by 1-4C alkyl, or by halogen, or by a CN or CF3 gp.; one of R2 and R'2 is OH and the other is morpholino, piperidino or NR3R4; R3 and R4 = 1-8C alkyl or 3-8C cycloalkyl, or one may be H. When R'2 = OH, then n = 2, R1 = 3,4-dimethylphenyl or 3,4-dichlorophenyl, and R2 = di(4-5C n-alkyl)amino. When R2 = OH, then n = 2, R1 = 4-cyanophenyl and R'2 = di(4-5C n-alkyl)amino.