反应详情

To a solution of 2-phenyl-pyrimidine-5-carboxylic acid (300 mg, 1.5 mmol) in DCM (10 mL) is added 1-[3-(dimethylamino)propyl-3-ethylcarbodiimide (316 mg, 1.65 mmol) and N-hydroxybenzotriazole (223 mg, 1.65 mmol) at rt and the mixture is stirred for 10 min. 4-Amino-4H-1,2,4-triazole (252 mg, 3 mmol) is added and the mixture is stirred at rt for 3 days. The resulting precipitate is filtered, washed with DCM and water, and dried in vacuum oven at 40° C. overnight to afford 2-phenyl-pyrimidine-5-carboxylic acid [1,2,4]triazol-4-ylamide (270 mg) as a solid. MS: 267 (M+H); 1H NMR (300 MHz, DMSO): δ=7.59 (m, 3H), 8.50 (d, 2H), 8.84 (s, 2H), 9.36 (s, 2H). IC50=262.5 nM.

1. stirringthe mixture is stirred at rt for 3 days
2. filtrationThe resulting precipitate is filtered
3. washwashed with DCM and water
4. customdried in vacuum oven at 40° C. overnight