D- AND L-1,2,3,4-TETRAHYDRO-ISOQUINOLINE-1-CARBOXYLIC ACIDS AND THEIR DERIVATIVES CONTAINING URETHANE-TYPE N-PROTECTING GROUPS AS WELL AS A PROCESS FOR PREPARING THEM AND THE CORRESPONDING RACEMATES

摘要

The invention relates to new L- and D-1,2,3,4-tetrahydro-isoquinoline-1-carboxylic acids and their derivatives containing urethane-type N-protecting groups of the formula: R-O-CO, wherein R represents a linear or branched C1-6 alkyl group; a benzyl group optionally substituted with one or more halogen atoms, nitro, methyl or methoxy groups; a picolyl group or a 9-fluorenylmethyl group, and their salts, furthermore to a process for preparing these compounds and the corresponding racemates, which comprises condensing glyoxylic acid hydrate and 2-phenethylamine with an N-protecting group of the general formula: R'-O-CO, wherein R' represents a linear or branched C1-3 alkyl group; a benzyl group optionally substituted with one or more halogen atoms or nitro groups; a picolyl group or a 9-fluorenylmethyl group in trifluoroacetic acid or in a halogenated hydrocarbon containing trifluoroacetic acid.