反应详情

To 4-bromophenyl acetylchloride (300 mg, 1.28 mmol) in CH2Cl2 (5 mL) was added 3-(tert-Butyl-diphenyl-silanyloxy)-azetidine (399 mg, 1.28 mmol), DIPEA (670 μL, 3.85 mmol) and the reaction stirred at RT for 2 h. The crude material was purified by silica gel column chromatography, eluting with isohexane and increasing the polarity to 80% EtOAc/isohexane to obtain 2-(4-bromo-phenyl)-1-[3-(tert-butyl-diphenyl-silanyloxy)-azetidin-1-yl]-ethanone as a colourless glass (632 mg, 97%).

1. customThe crude material was purified by silica gel column chromatography
2. washeluting with isohexane
3. temperatureincreasing the polarity to 80% EtOAc/isohexane