反应详情

4,6-Dichloro-5-fluoro-2-methylpyrimidine (100 mg, 0.55 mmol) was dissolved in 2 mL of DMSO and stirred at room temperature. Pyrrolidine (50 μL, 0.61 mmol) was added, followed by DIPEA (210 μL, 1.21 mmol). The resulting reaction mixture was stirred for 2 h, and then hydrazine was added (1.0 mL) and the contents were heated to 80° C. for 1 h. The reaction mixture was then cooled to room temperature and purified by RP-HPLC to provide 5-fluoro-4-hydrazino-2-methyl-6-(1-pyrrolidinyl)pyrimidine (69 mg, 59%).

1. customThe resulting reaction mixture
2. stirringwas stirred for 2 h
3. temperaturethe contents were heated to 80° C. for 1 h
4. temperatureThe reaction mixture was then cooled to room temperature
5. custompurified by RP-HPLC