Patent ID: 9656964
Date: 2017-05-23
CPC Classifications: A61P,C07D

Claim:
1. Process for the preparation of carboxamide derivatives of formula (I) wherein R is selected from the list of 2-isopropyl, 2-cyclopropyl, 2-tert-butyl, 5-chloro-2-ethyl, 5-chloro-2-isopropyl, 2-ethyl-5-fluoro, 5-fluoro-2-isopropyl, 2-cyclopropyl-5-fluoro, 2-cyclopentyl-5-fluoro, 2-fluoro-6-isopropyl, 2-ethyl-5-methyl, 2-isopropyl-5-methyl, 2-cyclopropyl-5-methyl, 2-tert-butyl-5-methyl, 5-chloro-2-(trifluoromethyl), 5-methyl-2-(trifluoromethyl), 2-chloro-6-(trifluoromethyl), 3-chloro-2-fluoro-6-(trifluoromethyl) and 2-ethyl-4,5-dimethyl, characterized in that 1-methyl-3-difluormethyl-5-fluoro-1H-pyrazole-4-carbonyl halides of the formula (II) in which Hal is F, Cl or Br, are reacted with amine derivatives of the formula (III) or (IY) in which R is as defined above, X is F, Cl, Br, J, HSO 4 , CH 3 COO, BF 4 , CH 3 SO 3 , CF 3 COO or CF 3 SO 3 , in the absence of an acid acceptor other than an amine of formula (III) or (IY), and wherein between 0.8 and 1.5 mol of amine derivatives are used per mol of the compound of formula (II).