反应详情

To {3-{[tert-butyl(diphenyl)silyl]oxy}-1-[4-(1-{[2-(trimethylsilyl)ethoxy]methyl}-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrazol-1-yl]cyclobutyl}acetonitrile (2.0 g, 3.0 mmol, a mixture of diastereomers from Step A) ethanol (82 mL) was added 5.0 M sodium hydroxide in water (9 mL, 50 mmol). The reaction was stirred overnight. The reaction mixture was diluted with water and ethanol was removed in vacuo. The aqueous mixture was extracted with ethyl acetate (3×). The combined organic extracts were washed with water, then brine, dried over sodium sulfate, decanted and concentrated. The product, as a mixture of diastereomers, was used without further purification in Step C. LCMS (M+H)+: 424.2.

1. customwas removed in vacuo
2. extractionThe aqueous mixture was extracted with ethyl acetate (3×)
3. washThe combined organic extracts were washed with water
4. dry with materialbrine, dried over sodium sulfate
5. customdecanted
6. concentrationconcentrated
7. additionThe product, as a mixture of diastereomers
8. customwas used without further purification in Step C