AMINO ACID DERIVATIVES AND A PROCESS FOR THE PREPARATION THEREOF

摘要

Novel compounds of the general formula (I), (I) and their salts and optically active isomers have been prepared. The new compounds according to the invention possess valuable pharmacological and therapeutical properties. In the above formula A1 stands for hydroxy, C1-4 alkoxy, cycloalkoxy, aralkoxy, substituted aralkoxy, aryloxy, substituted aryloxy or a group of the general formula -NR?4 or wherein R14 is hydrogen, C1-4 alkyl or aralkyl, R6 is hydrogen, C1-5 alkyl, aralkyl, hydroxyl-substituted aralkyl, heteroaralkyl or a group of the general formula Y is hydroxy, amino, alkylamino, dialkylamino, C1-4 alkoxy or aralkoxy, and r is an integer of from 1 to 10 or an average polymerization grade of up to 2000, B1 is a group of the formula -SO2OH, -OSO2OH, -O-PO(OH)2 or -S-S-R-11, wherein R11 is C1-4 alkyl, aralkyl or aryl or a residue obtained when removing group B1 from the general formula (I), R stands for hydrogen, C1-4 alkyl or aralkyl, R? stands for hydrogen or halogen, R1 stands for hydrogen C1-4 alkyl, aryl, aryl having a nitro or alkoxy substituent, aralkyl, substituted aralkyl, alkoxycarbonyl, aralkoxycarbonyl, aralkoxycarbonyl having a halogen, alkoxy, nitro, phenylaso, or alkoxyphenylaso substituent, alkyl-substituted aryloxycarbonyl, acyl, benzoyl, arylsulfonyl or -(NH-??-CO)p group (wherein R6 has the same meanings as defined above and p is an integer of from 1 to 10 or an average polymerization grade of up to 2000), or a -CO- group, R2 stands for hydrogen, C1-4 alkyl, aralkyl or a -CO- group, but if R1 and R2 each stand for a -CO- group, they form a ring through an o-phenylene, alkylene or -CH=CH- group, R3 stands for hydrogen, carboxy or carbalkoxy, R4 stands for hydrogen, halogen C1-4 alkyl or hydroxy, R5 stands for hydrogen, halogen, C1-4 alkyl, carboxy, carboxamino, carbalkoxy or carboaralkoxy, n is 1, 2 or 3, n is 1, 2, or 4, s is 0, 1, 2, 3 or 4, and t is 1, 2 or 3.