| 摘要 |
<p>The invention relates to a method of obtaining compounds having general formula 1 which includes racemic mixtures (¦)-1 and the enantiomerically pure compounds (-)-1 y (+)-1. In said formula, R1 and R3, which may be identical or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, on the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group. The preparation method consists in producing the racemic mixture having general formula (¦)-1 by reacting an (E)-1,1,1-trifluorine-4-aryl-3-butene-2-one with a phenylhydrazine followed by treatment with chlorosulphonic acid, or by reaction with chlorosulphonic acid followed by reaction with sodium hydroxide and, finally, with thionyl chloride. The product obtained by any of the aforementioned methods is made to react with ammonium or ammonia carbonate or with sodium sulphite and methyl iodide or methyl sulphate. Moreover, in order to produce enantiomerically pure compounds having general formula 1 by resolution of the racemic mixture having general formula (¦)-1, a reaction is carried out with optically-active ephedrine, followed by the formation of the sodium salt of each of the enantiomers, reaction with thionyl chloride and ammonium or ammonia carbonate, or with thionyl chloride followed by sodium sulphite and methyl iodide or methyl sulphate in order to produce separately the enantiomerically pure compounds having general formula (-)-1 y (+)-1.</p> |
