反应详情

2-(4-Fluoro-phenyl)-5-iodo-6-(methanesulfonyl-methyl-amino)-furo[2,3-b]pyridine-3-carboxylic acid methylamide (10 mg, 0.020 mmol), acrylonitrile (1.371 mg, 0.026 mmol), palladium(II) acetate (0.446 mg, 1.987 μmol) and triethylamine (2.77 μl, 0.020 mmol) in DMF (1 ml) were heated under microwave irradiation at 120° C. for 40 min. After LCMS showed predominant conversion to product, the reaction mixture was concentrated to dryness, taken up in DMF, filtered and purified by HPLC to afford the title compound (6 mg, 0.014 mmol, 70.5% yield). MS (ESI) m/z 429.3 (M+1). NMR (400 MHz, CD3CN) δ 8.51 (s, 1H), 8.06-8.03 (m, 2H), 7.94-7.89 (d, 1H, J=17 Hz), 7.34-7.30 (m, 2H), 6.91 (br s, 1H), 6.30-6.26 (d, 1H, J=17 Hz) (s, 1H), 3.31 (s, 3H), 3.12 (s, 3H), 2.91-2.89 (d, 3H).

1. concentrationthe reaction mixture was concentrated to dryness
2. filtrationfiltered
3. custompurified by HPLC