3-(2-Chloro-6-fluorophenyl)-5-methylisoxazole-4-carbonyl chloride → [1-(3,5-bis-trifluoromethyl-benzyl)-5-phenyl-1H-[1,2,3]triazol-4-yl]-[3-(2-chloro-6-fluorophenyl)-5-methyl-isoxazol-4-yl]-methanone

Participants

Reaction Steps

Heat a mixture of 3-(2-chloro-6-fluoro-phenyl)-5-methyl-isoxazole-4-carbonyl chloride (187 mg, 0.681 mmol) and 1-(3,5-bis-trifluoromethyl-benzyl)-4-(tri-n-butylstannanyl)-5-phenyl-1H-[1,2,3]triazole (300 mg, 0.454 mmol) in the presence of PdCl2(PPh3)2 (32 mg) in degassed 1,4-dioxane (3.0 mL) at 80° C. After 18 h., concentrate in vacuo and purify the residue by chromatography on silica gel to provide the title compound (50% yield) as a light yellow foam. MS (ES) 609.0 (M++1); TLC Rf=0.1 (6% acetone in hexanes).

Provenance & Evidence