反应详情

A solution of 6-bromo-3-bromomethyl-1,2-benzisoxazole (Intermediate 1, 130 mg), serinol (50 mg) and DIPEA (0.05 ml) in DMF (0.2 ml) was stirred at 60° under nitrogen for 3 h. The mixture was partitioned between water and ethyl acetate and the organic layer was washed with water and brine, dried through a hydrophobic filter and concentrated. The residue was purified on a Varian Bond Elut SPE cartridge (silica, 2 g) eluting with dichloromethane followed by dichloromethane-methanol (9:1) to give the title compound as a yellow gum (33 mg).

1. customThe mixture was partitioned between water and ethyl acetate
2. washthe organic layer was washed with water and brine
3. customdried through
4. filtrationa hydrophobic filter
5. concentrationconcentrated
6. customThe residue was purified on a Varian Bond Elut SPE cartridge (silica, 2 g)
7. washeluting with dichloromethane