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

Claim 1

A 1,2,3,4-Tetrahydroisoquinoline having the formula: ##SPC11## wherein R 1 and R 2 are each hydrogen or lower alkyl, R 3 is a triazolyl or tetrazolyl, each of which is substituted with up to one lower alkyl group, R 4 and R 5 are each hydroxy or a protected hydroxy, wherein the hydrogen atom is replaced by a member selected from the group consisting of acyl, lower alkyl, allyl, aryl, ar(lower) alkyl tetrahydropyranyl, methoxymethyl, 2-nitrophenylthio, 2, 4-dinitrophenylthio, and the combination wherein R 4 and R 5 together form a lower alkylenedioxy group, and X is --O-- or --S--, and pharmaceutically acceptable salts thereof, wherein "lower" refers to 1-6 carbon atom(s), aryl refers to phenyl, tolyl, xylyl, or naphthyl and acyl refers to benzyloxycarbonyl, 4-nitrobenzyloxycarbonyl, 4-bromobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, 3,4-dimethoxybenzyloxycarbonyl, 4-(phenylazo)benzyloxycarbonyl, 4-(4-methoxyphenylazo) benzyloxycarbonyl, tertiary-butoxycarbonyl, 1,1-dimethylpropoxycarbonyl, isopropoxycarbonyl, diphenylmethoxycarbonyl, 2-pyridylmethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl, 2,2,2-tribromoethoxycarbonyl, 3-iodopropoxycarbonyl, 2-fufuryloxycarbonyl, 1-adamantyloxycarbonyl, 1-cyclopropylethoxycarbonyl, 8-quinolyloxycarbonyl, methanesulfonyl, benzenesulfonyl, p-toluenesulfonyl, formyl, acetyl, benzoyl, toluoyl, phenylacetyl, trifluoracetyl or phenoxyacetyl.