反应详情

A mixture of trans-4-(4-indazol-1-ylpyrimidin-2-ylamino)-cyclohexanecarboxylic acid (100 mg, 0.30 mmol), 2-amino-2-butanol (39.2 mg, 0.44 mmol), BOP (194.6 mg, 0.44 mmol), DIPEA (77.4 mg, 0.60 mmol) in THF (8 mL) was stirred at RT overnight. Water (20 mL) was added to the resulting suspension: the solids first dissolved, then precipitated with the addition of more water (100 mL). The precipitate was collected by filtration, washed with water and Et2O, and dried under reduced pressure to give trans-4-(4-indazol-1-yl-pyrimidin-2-ylamino)-cyclo-hexanecarboxylic acid (3-hydroxy-butyl)amide (78 mg) as white solid. MS=409 [M+H]+.

1. dissolutionthe solids first dissolved
2. customprecipitated with the addition of more water (100 mL)
3. filtrationThe precipitate was collected by filtration
4. washwashed with water and Et2O
5. customdried under reduced pressure