1,1'-Carbonyldiimidazole → 5-[3-(2-Fluoro-4-iodo-phenylamino)-pyridin-4-yl]-3H-[1,3,4]oxadiazol-2-one

Participants

Reaction Steps

To a solution of 3-(2-Fluoro-4-iodo-phenylamino)-isonicotinic acid hydrazide (152 mg, 0.41 mmol) in THF (6 mL) contained TEA (60 μl, 0.43 mmol) were added Di-imidazol-1-yl-methanone (95 mg, 0.57 mmol) at 0° C. The reaction mixture was warmed to RT and stirred for 5 h, additional TEA (40 μl) and CDI (50 mg) were added, and the reaction mixture was stirred overnight at RT. The precipitate was filtered, the solid washed with MeOH. Yield: yellow solid 123 mg. LC-MS (Method A) [5.50 min; 399(M+1)].

Provenance & Evidence