反应详情

1-Benzyl-3-hydroxymethyl-4-hydroxypyrrolidine (66.2 g) and triethylamine (38.8 g) are added to dry dichloromethane (700 ml) and the mixture is cooled till a temperature of from -5° to -10° C. At this temperature, methanesulfonyl chloride (36.6 g) is added dropwise to the mixture with stirring. After the addition, the mixture is stirred for 30 minutes, and then washed with an aqueous sodium hydrogen carbonate and subsequently with water. Thereafter, the dichloromethane layer is separated, dried and concentrated to give 1-benzyl-4-hydroxy-3-methanesulfonylmethylpyrrolidine (80.8 g) as an oil.

1. temperaturethe mixture is cooled till a temperature of from -5° to -10° C
2. additionAfter the addition
3. stirringthe mixture is stirred for 30 minutes
4. washwashed with an aqueous sodium hydrogen carbonate and subsequently with water
5. customThereafter, the dichloromethane layer is separated
6. customdried
7. concentrationconcentrated