| abstract |
Fluorinated Amino acids and amines, compositions and process for preparing said compounds. n a-Difluoromethyl-3,4- di-OR-phenylalanines and its esters, and (1-difluoromethyl)- and 1-(trifluoromethyl)-2-(3,4-di-OR- phenyl) ethylamines, wherein R is hydrogen or a C 2 -C 6 alkanoyl, have been prepared. n Homoveratric acid is transformed into veratryl- difluoromethyl- ketone or veratryl- trifluoro- methyl- ketone, this reacts with methoxyamine, and the obtained O-methyl-oxime is reduced to the amine. The 3- and 4-methoxygroups are hydrolysed into hydroxy-groups. n Reaction of veratryl- difluoromethylketone with ammonium-carbonate and sodium cyanide yields a-difluoromethyl -5-(3',4'- dimethoxybenzyl)-2,4-imidazolidine-dione, hydrolysis results in α-difluoromethyl-3- hydroxytyrosine. The compounds have Dopa-decarboxylase inhibiting activity and some of them are antihypertensive agents. |