反应详情

A mixture of 1-methyl-5-(2-morpholino-[1,2,4]triazolo[1,5-a]pyridin-7-ylcarbamoyl)-1H-pyrazole-4-carboxylic acid (100 mg, 269 μmol), morpholine (141 μl, 1.62 mmol) and propylphosphonic anhydride (50% in ethyl acetate, 397 μl, 673 μmol) in tetrahydrofurane (7 ml) is refluxed for 18 hours. The solvent is evaporated, the residue diluted with ethyl acetate and washed with sat. aqueous sodium hydrogencarbonate solution and with water. The organic layer is dried with magnesium sulfate and the solvent removed in vacuo affording 1-Methyl-4-(morpholine-4-carbonyl)-N-(2-morpholino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1H-pyrazole-5-carboxamide (94 mg, 79.3%) as a light yellow solid. Mp.: 206-8° C. MS: m/z=441.3 (M+H+).

1. temperatureis refluxed for 18 hours
2. customThe solvent is evaporated
3. additionthe residue diluted with ethyl acetate
4. washwashed with sat. aqueous sodium hydrogencarbonate solution and with water
5. dry with materialThe organic layer is dried with magnesium sulfate
6. customthe solvent removed in vacuo