METHOD FOR PRODUCING 4- (2-CHLORO-4-METHOXY-5-METHYLPHENYL) -5-METHYLTHIAZOL-2-IL - 2-CYCLOPROPYL-1- (3-fluoro-4-methylphenyl) -ethyl -AMINE

摘要

1. The method of obtaining [4- (2-chloro-4-methoxy-5-methylphenyl) -5-methylthiazolo-2-yl] - [2-cyclopropyl-1- (3-fluoro-4-methylphenyl) ethyl] - an amine of formula (I) wherein: a) a compound of general formula (II) wherein X is halogen is reacted with an alkali metal thiocyanate in the presence of a phase transfer catalyst, and b) the 2-thiocyanate-1- (2-chloro-4 thus obtained) -methoxy-5-methylphenyl) propan-1-one of the formula (III) or its tautomeric form is reacted with 2-cyclopropyl-1- (3-fluoro-4-methylphenyl) ethylamine of the formula (IV) 2. A method according to claim 1, characterized in that in step b) a ketone of formula (III) is added to an amine of formula (IV). The method according to claim 2, characterized in that the addition of a ketone of the formula (III) to the amine of the formula (IV) is carried out for at least 1 hour. A method according to any one of claims 1 to 3, characterized in that in step a) the reaction is carried out in a binary system consisting of an aprotic solvent and water. The method according to claim 1, characterized in that stage b) is carried out in a non-polar aprotic solvent. The method according to claim 5, characterized in that the non-polar aprotic solvent used in step b) is methylcyclohexane or toluene. The method according to claim 1, characterized in that stage b) is carried out at a temperature of from 25 ° C to reflux temperature. The method according to claim 7, characterized in that stage b) is carried out at a reflux temperature. The method according to claim 1, characterized in that in the general formula (II) X is bromo. 10. 2-thiocyanate-1- (2-chloro-4-methoxy-5-methylphenyl) propan-1-one formulas (III) and its tautomers. 11. The tautomer of the compound of formula (III) according to claim 10, which is 5- (2-chloro-4-methoxy-5-methylphenyl) -4-methyl- [1.3] -oxathiol-2-ylideneamine of the formula (V) 12. The method of obtaining 2-thiocyanate-1- (2-chloro-4-meth�