反应详情

To a solution of [5-(Benzhydrylidene-amino)-pyridin-3-yl]-[7-bicyclo[1.1.1]pent-1-yl-2-(4-methoxy-benzylamino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-methanone (Preparation 286, 475 mg, 0.78 mmol) in THF (15 mL), citric acid (15 mL of a 1N aq. solution) was added at room temperature and the reaction mixture stirred for 2 hours. The reaction was then quenched with sat. aq. Na2CO3 solution and extracted with EtOAc (2×25 mL). The combined organic phases were dried (Na2SO4) and evaporated in vacuo. Purification by column chromatography on neutral alumina (Methanol:DCM 3:97) to afford the title compound as a pale yellow solid in 92% yield, 320 mg.

1. customThe reaction was then quenched with sat. aq. Na2CO3 solution
2. extractionextracted with EtOAc (2×25 mL)
3. dry with materialThe combined organic phases were dried (Na2SO4)
4. customevaporated in vacuo
5. customPurification by column chromatography on neutral alumina (Methanol:DCM 3:97)