反应详情

A mixture 2-methyl-6,7,8,9-tetrahydro-5H-[1,3]oxazolo[4,5-h][3]benzazepine (1 mmol), chloroacetaldehyde (2 mmol), NaBH(OAc)3 (2 mmol) in dry DME (10 ml) was stirred at room temperature for 3 h. The mixture was partitioned between aqueous Na2CO3 (0.5 M) and DCM. The organic layer was collected and the aqueous phase extracted twice with DCM. The combined DCM layers were concentrated and submitted to column chromatography (EtOAc—acetone gradient) to provide the title compound (36% yield).

1. customThe mixture was partitioned between aqueous Na2CO3 (0.5 M) and DCM
2. customThe organic layer was collected
3. extractionthe aqueous phase extracted twice with DCM
4. concentrationThe combined DCM layers were concentrated