反应详情

To a solution of (S)-methyl 2-(5-(4-(allyloxy)-4-methylpiperidin-1-yl)-2-(2′-hydroxy-5′-methyl-[1,1′-biphenyl]-3-yl)-7-methylimidazo[1,2-a]pyridin-6-yl)-2-(tert-butoxy)acetate (51 mg, 0.083 mmol, 1 equiv), (R)-pent-4-en-2-ol (22 mg, 0.250 mmol, 3 equiv), and PPh3 (44 mg, 0.167 mmol, 2 equiv) in THF (0.8 mL) was added DEAD (0.066 mL of a 40% solution in toluene, 0.167 mmol, 2 equiv). After stirring 18 h, the yellow solution was diluted with ether, washed with water, dried (MgSO4), and concentrated in vacuo. The crude product was purified by flash column chromatography (0-100% EtOAc [2% TEA]/hexane) to provide the product (53 mg, 94%) as a colorless film. LCMS (ESI, M+1): 680.45.

1. washwashed with water
2. dry with materialdried (MgSO4)
3. concentrationconcentrated in vacuo
4. customThe crude product was purified by flash column chromatography (0-100% EtOAc [2% TEA]/hexane)