反应详情

温度

50 °C

A mixture of 2-fluoro-4-[1-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-2-yl)-2-(tetrahydro-pyran-4-yl)-vinyl]-benzoic acid methyl ester (250 mg, 0.63 mmol) and 10% palladium on activated carbon (75 mg) in methanol (250 mL) was heated at 50° C. under hydrogen (50 psi) for 16 h. The mixture was cooled to 25° C., the solids filtered off, washed with ethyl acetate and concentrated in vacuo to afford 2-fluoro-4-[1-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-2-yl)-2-(tetrahydro-pyran-4-yl)-ethyl]-ethyl]-benzoic acid methyl ester (230 mg, 91%) which was used in the next step without further purification: LC/MS m/e calcd for C22H22F2N2O3 [M+H]+ 401.43, observed 400.9.

1. temperatureThe mixture was cooled to 25° C.
2. filtrationthe solids filtered off
3. washwashed with ethyl acetate
4. concentrationconcentrated in vacuo