EP 0000034 B1 19840523 - FLUORINATED AMINES, COMPOSITIONS AND PROCESS FOR PREPARING SAID COMPOUNDS
Title (en)
FLUORINATED AMINES, COMPOSITIONS AND PROCESS FOR PREPARING SAID COMPOUNDS
Publication
Application
Priority
US 80238877 A 19770601
Abstract (en)
[origin: EP0000034A1] alpha -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 C2-C6 alkanoyl, have been prepared. 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. Reaction of veratryl- difluoromethylketone with ammonium-carbonate and sodium cyanide yields alpha -difluoromethyl-5-(3 min , 4 min -dimethoxybenzyl)-2,4-imidazolidine-dione, hydrolysis results in alpha -difluoromethyl-3- hydroxytyrosine. The compounds have Dopa-decarboxylase inhibiting activity and some of them are antihypertensive agents.
IPC 1-7
IPC 8 full level
A61K 31/135 (2006.01); A61K 31/195 (2006.01); A61K 31/215 (2006.01); A61P 9/12 (2006.01); A61P 43/00 (2006.01); C07C 45/48 (2006.01); C07C 49/255 (2006.01); C07C 67/00 (2006.01); C07C 219/28 (2006.01); C07C 227/00 (2006.01); C07C 227/24 (2006.01); C07C 229/36 (2006.01); C07D 233/78 (2006.01)
CPC (source: EP)
A61P 9/12 (2017.12); A61P 43/00 (2017.12); C07C 45/48 (2013.01); C07C 49/255 (2013.01); C07D 233/78 (2013.01)
C-Set (source: EP)
Designated contracting state (EPC)
BE CH DE FR GB LU NL SE
DOCDB simple family (publication)
EP 0000034 A1 19781220; EP 0000034 B1 19840523; DE 2862407 D1 19840628; DK 240678 A 19781202; IE 47542 B1 19840418; IE 781077 L 19781201; IT 7849635 A0 19780531; JP S5416437 A 19790207
DOCDB simple family (application)
EP 78100057 A 19780601; DE 2862407 T 19780601; DK 240678 A 19780531; IE 107778 A 19780530; IT 4963578 A 19780531; JP 6501578 A 19780601