PROCESS FOR THE PREPARATION OF AMINOACID DERIVATIVES

摘要

RCOCR1R2NHCHR3CONR4CR5R7COR6 [R,R6 = OH, alkoxy, alkenoxy, dialkylaminoalkoxy, acyloxyalkoxy, (un)substituted alkoxy, NH2, dialkylamino, NHOH; R1 = H, C1-20 alkyl, substituted alkyl or Ph, heteroaralkyl, aralkenyl; R2R7 = H, alkyl; R3 = H, (un)substituted alkyl; R4 = H, alkyl; R5 = (un)substituted alkyl, Ph, phenylalkyl; NR4CR5 = (un)substituted ring were prepd. as antihypertensives and angiotensin-converting enzyme inhibitors. Thus, H-L-Ala-L-Pro-OH was condensed with PhCh2COCO2H in the presnece of NaBH3CH to give diastereometric PhCH2CH(CO2H)-L-Ala-L-Pro-OH.