反应详情

To a solution of 2-(4-(5-(2-cyclopentyl-6-methoxypyridin-4-yl)-1,2,4-oxadiazol-3-yl)-2-ethyl-6-methylphenoxy)ethanol (638 mg, 1.51 mmol) in THF, DIPEA (389 mg, 3.01 mmol) is added. The mixture is cooled to 0° C. before methanesulfonyl chloride (207 mg, 1.81 mmol) is added. The mixture is stirred at rt for 30 min before it is diluted with EA (100 mL) and washed with sat. aq. NaHCO3 solution (50 mL) and brine (50 mL). The org. extract is dried over MgSO4, filtered and concentrated to give 2-(4-(5-(2-cyclopentyl-6-methoxypyridin-4-yl)-1,2,4-oxadiazol-3-yl)-2-ethyl-6-methylphenoxy)ethyl methanesulfonate (733 mg) as a yellow oil; LC-MS: tR=1.19 min, [M+H]+=502.05.

1. additionis added
2. washwashed with sat. aq. NaHCO3 solution (50 mL) and brine (50 mL)
3. extractionextract
4. dry with materialis dried over MgSO4
5. filtrationfiltered
6. concentrationconcentrated