反应详情

A suspension of methyl 3-{(5S,7S)-7-[(6-cyano-1H-benzimidazol-1-yl)methyl]-2-oxo-1-oxa-3-azaspiro[4.5]dec-3-yl}-2,2-dimethylpropanoate (1.06 g, 2.505 mmol) and potassium trimethylsilanolate (0.482 g, 3.76 mmol) in THF (12.5 mL) was stirred at RT overnight. LCMS showed the reaction was not complete. Additional potassium trimethylsilanolate (0.482 g, 3.76 mmol) was then added, and the reaction was stirred for one additional day. The reaction mixture was then concentrated to a light yellow solid. The solid was washed with a mixture of DCM and Et2O and dried under vacuum to give 3-{(5S,7S)-7-[(6-cyano-1H-benzimidazol-1-yl)methyl]-2-oxo-1-oxa-3-azaspiro[4.5]dec-3-yl}-2,2-dimethylpropanoic acid as a light yellow solid. This product was used in the next step without any further purification. MS (m/z) 411.2 (M+H+).

1. stirringthe reaction was stirred for one additional day
2. concentrationThe reaction mixture was then concentrated to a light yellow solid
3. washThe solid was washed with a mixture of DCM and Et2O
4. customdried under vacuum