反应详情

The mixture of (3R)-(−)-1-benzyl-pyrrolidin-3-ylamine (10 mmol, 1.76 g), bis(2-chloroethyl)ether (11 mmol, 1.29 mL), K2CO3 (40 mmol, 5.52 g) and NaI (0.4 mmol, 60 mg) in CH3CN (100 mL) was heated at reflux for 36 h under N2. It was then absorbed on silica gel (10 g) and evaporated to dryness. The solid was loaded on silica gel column and subjected to flash chromatograph (CH2Cl2/CH3OH=60/1-20/1). (3R)-1-(1-benzyl-pyrrolidin-3-yl)-piperidine 7 was obtained as white gum (1.4 g, 60%).

1. temperaturewas heated
2. temperatureat reflux for 36 h under N2
3. customIt was then absorbed on silica gel (10 g)
4. customevaporated to dryness