反应详情

2-(2-tert-Butylamino-3,5-dichloro-pyridin-4-yl)-1-{2-[2-(4-fluoro-phenyl)-ethoxy]-3,4-dimethoxy-phenyl}-ethanone obtained from example 300 (16.5 mg, 0.0308 mmol), triethylsilane (2 eq.) and TFA (0.1 mL) in dichloroethane (0.2 mL) was heated to 50° C. for 24 hours. The crude mixture was evaporated in vacuo, redissolved in dichloroethane (1 mL) and washed with NaHCO3 (sat, 2×0.5 mL). The organic phase was dried over Na2SO4 and the solvent evaporated in vacuo. Pure 2-(2-amino-3,5-dichloro-pyridin-4-yl)-1-{2-[2-(4-fluoro-phenyl)-ethoxy]-3,4-dimethoxy-phenyl}-ethanone was obtained by flash chromatography using a gradient of MeOH in dichloromethane as eluent.

1. customThe crude mixture was evaporated in vacuo
2. dissolutionredissolved in dichloroethane (1 mL)
3. washwashed with NaHCO3 (sat, 2×0.5 mL)
4. dry with materialThe organic phase was dried over Na2SO4
5. customthe solvent evaporated in vacuo