NEW MATERIAL:A compound expressed by formula I [R1 is alkoxycarbonyl, alkoxycarbonylamino or formula II (A is single bond, alkylene, etc.; Ra is CN, alkyl, aryl, etc.), etc.; R2 is phenyl or naphthyl; R3 is alkyl, cyclohexyl or phenyl; R4 is COORc (Rc is alkyl) or formula III (Ra is heterocyclic group; n is 0-2); R5 is H or alkyl] and salts thereof.
EXAMPLE: (2RS,3S)-3-(N-tert-Butoxycarbonyl-L-phenylalanyl-L-histidylamino)-5- methyl-1-[(1-methyl-5-tetrazolyl)thio]-2-hexanol.
USE: A renin inhibitor useful as a preventive and treating agent for hypertension.
PREPARATION: An N-[2-substituted-3-substituted propionyl]histidine expressed by formula IV or a C-terminal activated substance thereof is reacted with a 3-amino-1-substituted thio-2-substituted-4-substituted butane expressed by formula V to afford the compound expressed by formula I.
FUJIKURA TAKASHI
HARA RYUICHIRO
ICHIHARA MASATO
FUKUNAGA YUKIKO
SHIBAZAKI MASAYUKI
