反应详情

温度

70 °C

Ethyl 2,2-difluoroacetate (0.43 ml, 4.10 mmol) and hydrazine monohydrate were heated to 60° C. in N,N-dimethylformamide (1 ml) for 30 minutes to give a colourless solution. Tert-butyl (1-(4-(7-phenyl-2-thioxo-2,3-dihydro-1H-pyrido[2,3-b][1,4]oxazin-6-yl)phenyl)cyclobutyl)carbamate (100 mg, 0.205 mmol) was added to the previous solution at room temperature. The resulting mixture was heated to 70° C. for 20 hours. The reaction mixture was concentrated under reduced pressure and the crude material (100 mg, quantitative yield) was used for the next step without further purification. LCMS (Method D): RT=1.37 min, M+1=564.

1. customto give a colourless solution
2. concentrationThe reaction mixture was concentrated under reduced pressure