反应详情

温度

130 °C

A solution of (S)-tert-butyl 3-(6-bromo-3-carbamoylpyrrolo[1,2-b]pyridazin-4-ylamino)piperidine-1-carboxylate (75 mg, 0.17 mmol), phenylboronic acid (31.3 mg, 0.26 mmol), and PdCl2(dppf) 6.3 mg, (0.009 mmol) in DMF (1.5 mL) was added aq. K3PO4 (2M, 0.26 mL) then heated at 130° C. for 25 min. The mixture was poured into ethyl acetate (with 20% heptane) and washed with water then sat. aq. NaHCO3. The organic layer was dried over Na2SO4, filtered and concentrated. The crude product was purified via column chromatography (50-75% ethyl acetate in heptane) to afford the title compound (63 mg, 85% yield). LCMS 436.16 (M+H)+; HPLC (conditions L): retention time=4.02 min.

1. washwashed with water
2. dry with materialThe organic layer was dried over Na2SO4
3. filtrationfiltered
4. concentrationconcentrated
5. customThe crude product was purified via column chromatography (50-75% ethyl acetate in heptane)