反应详情

温度

23 °C

To a suspension of 7-bromo-2-(3-ethyl-ureido)-[1,2,4]triazolo[1,5-a]pyridine-5-carboxylic acid ethyl ester (which may be produced as in Example 6) (0.080 g, 0.22 mmol) in dimethylsulfoxide (1 mL) was added pyrrolidine (0.2 mL). The reaction was stirred at 23° C. for 30 minutes then 80° C. for 3 days. The reaction was then diluted with water (2 mL), acidified with 1N aqueous hydrogen chloride, then neutralized with saturated aqueous sodium bicarbonate and extracted with ethyl acetate (3×20 mL). The combined organic extracts were dried over sodium sulfate and evaporated in vacuo to give a solid that was purified by silica gel chromatography (gradient elution: 0-20% isopropanol/dichloromethane) to give the title compound as a solid. MS (APCI)=372.2 [M+H]

1. wait80° C. for 3 days
2. extractionextracted with ethyl acetate (3×20 mL)
3. dry with materialThe combined organic extracts were dried over sodium sulfate
4. customevaporated in vacuo
5. customto give a solid
6. customthat was purified by silica gel chromatography (gradient elution: 0-20% isopropanol/dichloromethane)