反应详情

A mixture of 102b (0.773 g, 1.75 mmol), oxetan-3-one (0.189 g, 2.62 mmol), NaBH3CN (0.22 g, 3.5 mmol), and zinc chloride/Et2O (3.5 ml, 3.5 mmol) in methanol (40 mL) was stirred at 50˜60° C. for 5 hours. The solid was removed by filtration and the filtrate was concentrated under reduced pressure. The residue was purified by column chromatography eluting with 5:1 CH2Cl2/methanol to afford 102c (200 mg, 30%). MS: [M+H]+ 385.

1. customThe solid was removed by filtration
2. concentrationthe filtrate was concentrated under reduced pressure
3. customThe residue was purified by column chromatography
4. washeluting with 5:1 CH2Cl2/methanol