合成路线1

The cyclization of 3-bromophenylhydrazine (I) with 2-(trichloroacetyl)-3-methoxycrotonic acid (II) in refluxing ethanol gives, after chromatographic separation, 1-(3-bromophenyl)-3-methylpyrazole-5-carboxylic acid ethyl ester (III), which by reaction with CuCN in refluxing N-methylpyrrolidone is converted into the 3-cyanophenyl analogue (IV). The hydrolysis of (IV) with LiOH in THF/water affords the corresponding carboxylic acid (V), which by reaction with oxalyl chloride in dichloromethane gives the acyl chloride (VI). The condensation of (VI) with 2-(2-aminopyrimidin-4-yl)-N-tert-butylbenzenesulfonamide (VII) by means of TEA in dichloromethane provides the corresponding amide (VIII), which is finally treated first with HCl in methanol, and then with ammonium carbonate in the same solvent.