反应详情

4-Cyclopropyl-2-(5-(5-(isopropylamino)-1,3,4-oxadiazol-2-yl)-1-tosyl-1H-indol-3-yl)pyrimidine-5-carboxylic acid (107 mg, 0.192 mmol) was treated with PyBOP (169 mg, 0.326 mmol) and 1,4-dioxane (5 mL) and DMF (1.0 mL) and stirred at RT for 10 min. The reaction was then cooled in an ice bath and treated with NH3, 0.5 M solution in 1,4-dioxane (1.9 mL, 0.96 mmol) and stirred at 0° C. for 1.5 h. The reaction was quenched with water, extracted with EtOAc (25 mL), washed with brine (2×25 mL), dried over MgSO4, filtered and concentrated affording 261 mg of the crude amide. MS (ESI, pos. ion) m/z: 558.2 (M+H)+. The crude material was used without further purification.

1. temperatureThe reaction was then cooled in an ice bath
2. stirringstirred at 0° C. for 1.5 h
3. customThe reaction was quenched with water
4. extractionextracted with EtOAc (25 mL)
5. washwashed with brine (2×25 mL)
6. dry with materialdried over MgSO4
7. filtrationfiltered
8. concentrationconcentrated