摘要 |
<p>NEW MATERIAL:The compound of formula I [R1 is H, lower alkyl, acyl, lower alkoxycarbonyl, etc.; R2 is H, (substituted) lower alkyl, (substituted) aryl, etc.; R3 is H, lower alkyl, aralkyl, acyl, or lower alkoxycarbonyl; R4 is H or lower alkyl] and its salt. EXAMPLE:N-( N-t-Butoxycarbonyl-L-isoleucyl-L-phenylalanyl-( R )-(-)-1-amino-2-(4- benzyloxyphenyl)ethylphosphonic acid diethyl ester hydrochloride. USE:Antihypertension agent. PROCESS:The compound of formula I can be prepared, e.g. by reacting the compound of formula II [Y is amino-protecting group; R2' is (protected) R2] with the compound of formula III (R3' and R4' are R3 and R4 except H), eliminating the amino-protecting group, reacting the product with the compound of formula IV(R1' is R1 except H), and if necessary, removing the protecting groups from the product.</p> |