反应详情

温度

100 °C

At room temperature, NaH (71 mg, 2.94 mmol) was added to a solution of tert-butyl-3-hydroxypyrrolidine-1-carboxylate (1B2) (500 mg, 2.67 mmol) in THF (tetrahydrofuran) (10 mL) and stirred for 1 hour. 4-chloropyrimidin-5-amine (H) (348 mg, 2.67 mmol) was then added. The reaction mixture was then heated to 100° C. under nitrogen and stirred for 4 hours, cooled to room temperature (20-30° C.) and concentrated in vacuo. The residue was purified with flash column (eluent: 10-30% ethyl acetate/petroleum ether) to obtain the product 1D3 (336 mg, 1.2 mmol).

1. stirringstirred for 4 hours
2. temperaturecooled to room temperature (20-30° C.)
3. concentrationconcentrated in vacuo
4. customThe residue was purified with flash column (eluent: 10-30% ethyl acetate/petroleum ether)
5. customto obtain the product 1D3 (336 mg, 1.2 mmol)