Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids, salts thereof, pharmaceutical compositions containing the derivatives or salts, and the production of the same.

摘要

There are disclosed substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids having the following general formula:-
where R is a hydrogen atom or a lower alkyl or aralkyl radical; R¹ is a hydrogen atom or a lower alkyl or benzyl radical; R² is a hydrogen atom or a lower alkyl radical; Ar is a phenyl radical or a substituted phenyl radical having 1 or 2 substituents selected from fluorine, chlorine and bromine atoms and lower alkyl, lower alkoxy, hydroxy or amino radicals; X and Y are independently hydrogen atoms or lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl or hydroxy radicals, or X and Y together constitute methylenedioxy; m is 0,1,2 or 3; and lower alkyl and lower alkoxy radicals contain from 1 to 4 carbon atoms in a straight chain or branched chain; or a pharmaceutically acceptable salt of the compound of formula I.

The substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids and the pharmaceutically acceptable salts thereof may be produced by coupling a suitably substituted 1,2,3,4-tetrahydroisoquinoline with a suitably substituted amino acid and, when desired, hydrolysing or removing the protecting groups of the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.