反应详情

In pyridine (30 ml) is dissolved R-isomer-rich ethyl 6-(1-benzyloxycarbonyl-4-piperidyl)-2-hydroxyhexanoate (7 g), and methanesulfonyl chloride (2.9 ml) is added dropwise, with stirring, under ice-cooling over the period of 5 minutes. The mixture is stirred under ice-cooling for 1.5 hours, and water (5 ml) is added dropwise to the mixture. The reaction mixture is stirred for 30 minutes, diluted with ethyl acetate (300 ml) and washed with 1N hydrochloric acid, saturated sodium hydrogencarbonate solution and water. The ethyl acetate layer is dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give R-isomer-rich ethyl 6-(1-benzyloxycarbonyl-4-piperidyl)-2-methanesulfonyloxyhexanoate (8.2 g) as a pale yellow oil.

1. additionis added dropwise
2. temperaturecooling over the period of 5 minutes
3. stirringThe mixture is stirred under ice-
4. temperaturecooling for 1.5 hours
5. stirringThe reaction mixture is stirred for 30 minutes
6. washwashed with 1N hydrochloric acid, saturated sodium hydrogencarbonate solution and water
7. dry with materialThe ethyl acetate layer is dried over anhydrous magnesium sulfate
8. concentrationconcentrated under reduced pressure