反应详情

Compound methyl 3-(cyclopentylamino)-2,2-difluoropropanoate (400 mg, 2 mmol) was solubilized in acetone (20 mL, dry). The solution was cooled in an ice water bath under a nitrogen atmosphere and K2CO3 (552 mg, 4 mmol) added. To this, a solution of 2,4-dichloro-5-nitropyrimidine (407 mg, 2.1 mmol) in acetone (5 mL, dry) was added dropwise. The reaction mixture was warmed up to room temperature and stirred for 4 hr. After that, it was diluted with EtOAc and washed by brine and water. The organic extracts were dried over MgSO4, filtered and concentrated to yield methyl 3-((2-chloro-5-nitropyrimidin-4-yl)(cyclopentyl)amino)-2,2-difluoropropanoate which was used directly for next step without further purification. [M+H] calc'd for C13H15ClF2N4O4, 365; found 365.

1. temperatureThe solution was cooled in an ice water bath under a nitrogen atmosphere
2. washwashed by brine and water
3. dry with materialThe organic extracts were dried over MgSO4
4. filtrationfiltered
5. concentrationconcentrated