反应详情

A solution of 4-(3-trifluoromethanesulfonyl-phenylamino)-piperidine (731 mg, 237 mmol) and Et3N (0.5 mL, 3.58 mmol) in CH2Cl2 (20 mL) was treated with the diallylamino sulfonyl chloride 269b 23° C. A thick precipitate appeared within 5 min, and the mixture was stirred overnight (even if complete within minutes). Dilution with CH2Cl2 (50 mL), washing (1120; brine), drying (MgSO4), and evaporation afforded the crude product, which was filtered over silica gel (AcOEt:cyclohexane 1:1) to afford 1.15 g (86%) of the title bisallylamine, which was used in the next step without further purification.

1. washDilution with CH2Cl2 (50 mL), washing (1120; brine)
2. customdrying
3. custom(MgSO4), and evaporation
4. customafforded the crude product, which
5. filtrationwas filtered over silica gel (AcOEt:cyclohexane 1:1)