反应详情

To a solution of (±)-(cis)-7-bromo-8-fluoro-1,3,4,14b-tetrahydro-4-oxo-2H-dibenzo[b,f]pyrido[1,2-d][1,4]oxazepine-1-carboxylic acid (13.1 g, 32.3 mmol) in toluene (660 mL), triethylamine (7.6 mL, 54 mmol) and diphenyl phosphorazidate (9.1 mL, 42 mmol) were added. The reaction mixture was heated to reflux for 2 h. Subsequently, methanol (31.9 mL, 787 mmol) was added and stirring was continued for 2 h at 70 ° C. After cooling down to room temperature, the reaction mixture was dried over P.S. filter and evaporated, to give the crude title compound (30.5 g, 100%) which was used without further purification. (m/z)=435+437 (M+H)−.

1. temperatureThe reaction mixture was heated
2. temperatureto reflux for 2 h
3. customthe reaction mixture was dried over P.S
4. filtrationfilter
5. customevaporated