Fujisawa Pharmaceutical Company, Ltd.

Yoshiyuki Kaneda

Teiji Kishimoto

Hiromu Kochi

A 1,2,3,4-tetrahydroisoquinoline having smooth muscle relaxant activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl, R.sub.3 is phenyl having substituents selected from the group consisting of lower alkenyloxy, mercapto, lower alkylthio, sulfamoyl and mono or disubstituted sulfamoyl, or a heterocyclic group, R.sub.4 and R.sub.5 are each hydroxy or protected hydroxy and X is --O-- or--S--.

1,2,3,4-Tetrahydroisoquinoline derivatives and the preparation thereof

A 1,2,3,4-tetrahydroisoquinoline having smooth muscle relaxant activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl and X is --O-- or --S--, and pharmaceutically acceptable salts thereof.

A 1,2,3,4-tetrahydroisoquinoline having the formula: ##SPC1## Which has relaxing activity on smooth muscles.

The present invention relates to new 1,2,3,4-tetrahydroisoquinoline derivatives, which have relaxing activity on smooth muscles. The present invention also relates to the preparation of new and known 1,2,3,4-tetraydroisoquinoline derivatives.

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Osaka, Japan

Yoshiyuki Kaneda