Pivalic acid → 4''-[3-Butyl-5-oxo-1-(2-trifluoromethyl-phenyl)-1,5-dihydro-[1,2,4]triazol-4-ylmethyl]-biphenyl-2-sulfonic acid (2,2-dimethyl-propionyl)-amide

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Reaction Steps

The title compound was prepared from 5-n-butyl-2,4-dihydro-4-[(2'-sulfamoylbiphenyl-4-yl)methyl]-2-[2-(trifluoromethyl)phenyl]-3H-1,2,4-triazol-3-one (from Example 16, Step C), according to the procedure of Example 43 except that pivalic acid was used as the acid. Excess pivalic acid was removed by 10% aq. KHCO3. The crude product was purified by flash chromatography (gradient elution using 1-5% MeOH/CH2Cl2) to afford a 86% yield of the desired compound as a white solid, homogeneous by TLC in 5% MeOH/CH2C2 ; mass spectrum (FAB) m/e 615 (M+1)+ ; mp 176°-178° C.

Provenance & Evidence