反应详情

To a solution of 4-hydroxy-6-(trifluoromethyl)quinoline-2-carbonitrile (2 g, 8.4 mmol) from above step D, in dry dioxane was added TEA (2.9 mL, 21 mmol) and PyBroP (4.75 g, 10 mmol) and stirred at 50 C for 2 hour. To this solution tert-butyl 3-(2-aminoacetamido)azetidine-1-carboxylate (2.9 g, 12.45 mmol) from example 1, step E, was added and stirred at room temperature for 48 h. The solution was concentrated in vacuo. Water was added to the residue and extracted with EtOAc. The ethyl acetate was removed under vacuum and the residue was purified by flash chromatography (silica gel, 0 to 80% EtOAc in hexane) to give the title compound.

1. stirringstirred at room temperature for 48 h
2. concentrationThe solution was concentrated in vacuo
3. additionWater was added to the residue
4. extractionextracted with EtOAc
5. customThe ethyl acetate was removed under vacuum
6. customthe residue was purified by flash chromatography (silica gel, 0 to 80% EtOAc in hexane)