反应详情

0.5 g of 3-[4-(2-tert-Butyl-6-cyclopropyl-pyrimidin-4-yl)-piperazin-1-yl]-propan-1-ol (1.57 mmol) were dissolved in 5 ml of tetrahydrofuran. 1.5 ml of n-butyllithium (15% in hexane) were added to the mixture at 0° C. Stirring was continued for 30 min and then 0.45 g of 4-benzyloxy-2-methanesulfonyl-pyrimidine (1.7 mmol) dissolved in 5 ml of tetrahydrofuran were added. The reaction was stirred overnight at room temperature and for an additional 2 h at 40° C. The reaction mixture was partitioned between water and ethyl acetate. The organic layer was dried over magnesium sulfate, filtered, and the solvent was evaporated. The crude product was purified by chromatography on silica gel using dichloromethane-methanol (0-3%) as eluent to yield 0.6 g of the title compound.

1. additionwere added
2. stirringThe reaction was stirred overnight at room temperature and for an additional 2 h at 40° C
3. customThe reaction mixture was partitioned between water and ethyl acetate
4. dry with materialThe organic layer was dried over magnesium sulfate
5. filtrationfiltered
6. customthe solvent was evaporated
7. customThe crude product was purified by chromatography on silica gel