反应详情

n-BuLi (4.7 mL, 11.8 mmol, 2.5 M in hexane) was added to a solution of diisopropylamine (1.13 g, 11.2 mmol) in THF (20 mL) at −78° C. After stirring for 5 min, neat cyclobutanecarbonitrile (0.8 g, 9.87 mmol) was added and the mixture was stirred at −78° C. for 1 hour. Then a solution of Example 44A (2.6 g, 11.8 mmol) in THF (10 mL) was added and the mixture was stirred at −78° C. for 1 h. The mixture was quenched with water and extracted with EtOAc (40 mL). The solvent was evaporated and the residue was used directly in the next step without further purification. LC-MS: m/z 220 (M+H).

1. stirringthe mixture was stirred at −78° C. for 1 hour
2. stirringthe mixture was stirred at −78° C. for 1 h
3. customThe mixture was quenched with water
4. extractionextracted with EtOAc (40 mL)
5. customThe solvent was evaporated
6. customthe residue was used directly in the next step without further purification