反应详情

To a solution of 5-(4-chloro-phenyl)-1-(2-methoxy-phenyl)-3-(2,2,6,6-tetramethyl-tetrahydro-pyran-4-yl)-1H-pyrazole (Example 1) (105 mg, 0.25 mmol) in mL of DCM at −78° C. was added a 1M solution of boron tribromide (0.33 mL, 0.33 mmol) in DCM. After 1 hr at −78° C. the reaction was quenched with 3 mL of 1N HCl and then diluted with 50 mL of EtOAc. The organic layer was washed with 50 mL of NaHCO3 and brine, and dried over Na2SO4. The crude product was purified by silica gel chromatography (Thomson Scientific 12-g cartridge, 2-40% EtOAc in heptane in column volumes) to give 60 mg (59%) of the title compound as a white solid.

1. customAfter 1 hr at −78° C. the reaction was quenched with 3 mL of 1N HCl
2. additiondiluted with 50 mL of EtOAc
3. washThe organic layer was washed with 50 mL of NaHCO3 and brine
4. dry with materialdried over Na2SO4
5. customThe crude product was purified by silica gel chromatography (Thomson Scientific 12-g cartridge, 2-40% EtOAc in heptane in column volumes)