Derivatives of fluorophenacyl amines and their therapeutic use.

摘要

1. Claims (for the Contracting States : BE, CH, DE, GB, IT, LI, LU, NL, SE) A new compound belonging to the family of fluorophenacyl-amine derivatives of the formula see diagramm : EP0060954,P11,F1 [wherein A is CO or CHOH and R is CH(CH3 )2 or C(CH3 )3 ] said compound being characterized in that it is selected from the group consisting of N-(4-fluorophenacyl)-isopropylamine, N-(2-fluorophenacyl)-tertiobutylamine, 1-(2-fluorophenyl)-2-tertiobutylamino-1-ethanol, 1-(4-fluorophenyl)-2-tertiobutylamino-1-ethanol and their addition salts. 1. Claim (for the Contracting State AT) Process for the preparation of a derivative belonging to the family of fluorophenacylamine derivatives of the formula see diagramm : EP0060954,P11,F2 wherein A is CO or CHOH and R is CH(CH3 )2 or C(CH3 )3 selected from the group consisting of N-(4-fluorophenacyl)-isopropylamine, N-(2-fluorophenacyl)-tertiobutylamine, 1-(2-fluorophenyl)-2-tertiobutylamino-1-ethanol, 1-(4-fluorophenyl)-2-tertiobutylamino-1-ethanol and their addition salts, said process being characterized in that 1. a fluorophenacyl halide of formula see diagramm : EP0060954,P11,F3 wherein X1 is Cl or Br, is reacted with an amine of formula H2 NR wherein R is defined as above in an alcohol, for at least one hour at the reflux temperature of the reaction medium, to obtain a derivative of formula I wherein A is CO, and 2. the carbonyl derivative wherein A is CO thus obtained is reduced by means of NaBH4 to obtain a derivative of formula I wherein A is CHOH.