反应详情

To a solution of 1-(tert-butoxycarbonyl)-4-(2-hydroxyeth-1-yl)-4-(3-benzyl-(1H)-pyrazol-5-yl)piperidine (125 mg, 0.32 mmol) from Step I in THF (4 mL) at 0° C. was added triphenylphosphine (85 mg, 0.32 mmol) and DEAD (0.051 mL, 0.32 mmol). The reaction was stirred for 20 min and was then allowed to warm to room temperature for 2 h. The mixture was concentrated and purified by flash chromatography eluting with 80% ethyl acetate in hexanes, then 5% methanol in methylene chloride to afford the title compound (100 mg).

1. concentrationThe mixture was concentrated
2. custompurified by flash chromatography
3. washeluting with 80% ethyl acetate in hexanes