p-(Methylsulphonyl)benzoic acid → 5-n-Butyl-2,4-dihydro-4-[[2'-[N-[p-(methylsulfonyl)benzoyl]sulfamoyl]-biphenyl-4-yl]methyl]-2-[2-(trifluoromethyl)phenyl]-3H-1,2,4-triazol-3-one

関与物質

反応手順

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 p-(methylsulfonyl)benzoic acid was used as the acid. The crude product was purified by flash chromatography (gradient elution using 0.5-10% MeOH/CH2Cl2) to afford a 60% yield of the desired compound as a white solid, homogeneous by TLC in 5% MeOH/CH2Cl2 ; mass spectrum (FAB) m/e 735 (M+Na)+, 751 (M+K)+ ; mp 131°-133° C.

情報源と証拠