反应详情

To a mixture of 4-chloro-6-(trifluoromethyl)pyrimidine (0.82 g, 4.49 mmol) and Boc-4-aminopiperidine (1.17 g, 5.84 mmol) in NMP (5.7 mL) was added DIPEA (1.10 mL, 6.29 mmol) and after 30 minutes the mixture was poured into water and extracted with ethyl acetate. The combined organic phases were dried over sodium sulfate, filtered and evaporated. Purification by chromatography (silica gel, 70 g, 0 to 50% ethyl acetate in heptane) afforded the title compound (1.43 g, 92%) as a white solid. MS ISP (m/e): 347.2 [(M+H)+].

1. extractionextracted with ethyl acetate
2. dry with materialThe combined organic phases were dried over sodium sulfate
3. filtrationfiltered
4. customevaporated
5. customPurification by chromatography (silica gel, 70 g, 0 to 50% ethyl acetate in heptane)