| abstract |
NEW MATERIAL:The compound of formula I [R 1 is H, lower alkyl, acyl, lower alkoxycarbonyl, etc.; R 2 is H, (substituted) lower alkyl, (substituted) aryl, etc.; R 3 is H, lower alkyl, aralkyl, acyl, or lower alkoxycarbonyl; R 4 is H or lower alkyl] and its salt. n EXAMPLE: N-( N-t-Butoxycarbonyl-L-isoleucyl-L-phenylalanyl-( R )-(-)-1-amino-2-(4- benzyloxyphenyl)ethylphosphonic acid diethyl ester hydrochloride. n USE: Antihypertension agent. n PROCESS: The compound of formula I can be prepared, e.g. by reacting the compound of formula II [Y is amino-protecting group; R 2 ' is (protected) R 2 ] with the compound of formula III (R 3 ' and R 4 ' are R 3 and R 4 except H), eliminating the amino-protecting group, reacting the product with the compound of formula IV(R 1 ' is R 1 except H), and if necessary, removing the protecting groups from the product. n COPYRIGHT: (C)1984,JPO&Japio |