2-amino-tetrahydro-isoquinoline derivatives and a process...

C - Chemistry – Metallurgy – 07 – D

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C07D 217/00 (2006.01) A61K 31/47 (2006.01) C07D 217/08 (2006.01)

Patent

CA 1329209

A b s t r a c t The present invention relates to tetrahydro-isoquinoline derivatives of the general Formula (I) Image I. wherein R stands for hydrogen or chlorine R1 and R2 stand for hydrogen, methoxy or ethoxy R3 and R4 stand for hydrogen or methyl and a process for the preparation thereof as well as pharma- ceutical compositions containing as active ingredients isoquinoline derivatives of the general Formula (I). The compounds of Formula I are prepared by reacting a 2-amino- tetrahydro-isoquinoline derivative of the general Formula(II) Image II. wherein R1, R2, R3 and R4 are as given above - with a carboxylic acid derivative of the general Formula(III) Image III. wherein X stands for chlorine, -OH, -OCH2CN, -OCH3, -OC2H5, -OCOOCH3 or -OCOOC2H5 R5 and R6 stand for hydrogen or together form CHN(CH3)2 and in case of the general Formula (Ia) Image wherein R. R1, R2, R3 and R4 are as given above splitting off the protective group in alkaline medium. The compound of Formula (I) have diuretic or saluretic utility.

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