反应详情

To a solution of (R)-3-amino-1-N-Boc-piperidine (920 mg) in dry EtOH (20 mL) were added successively 5-bromo-2-chloropyrimidine (957 mg), DIEA (0.86 mL). The reaction mixture was stirred at reflux for 16 hours under nitrogen. After cooling to RT, the reaction mixture was diluted with EA, washed with sat. NaHCO3, 1N NaOH. The organic extract was dried (MgSO4), filtered and concentrated to yield a crude brown-orange oil. FC (EA/n-heptane: 2/8) gave 787 mg (48%) of the title compound as a light brown solid.

1. temperatureat reflux for 16 hours under nitrogen
2. washwashed with sat. NaHCO3, 1N NaOH
3. extractionThe organic extract
4. dry with materialwas dried (MgSO4)
5. filtrationfiltered
6. concentrationconcentrated
7. customto yield a crude brown-orange oil