反应详情

A mixture of Intermediate 23b (900 mg, 1.80 mmol), morpholine (240 mg, 2.70 mmol), potassium-tert-butoxide (303 mg, 2.70 mmol), 2-dicyclohexylphosphino-2′,4′,6′-triisopropyl biphenyl (87 mg, 0.18 mmol), and tris(dibenzylideneacetone)dipalladium(0) (81 mg, 0.09 mmol) in THF (9 mL) was irradiated in the microwave at 100° C. for 20 min. The reaction was diluted with water and extracted with EtOAc (×2). The combined organics were washed with brine, dried (MgSO4), filtered and evaporated in vacuo. The residue was purified by FCC, using 0-100% EtOAc in cyclohexane, to give the title compound (290 mg, 40%). LCMS (Method 7): Rt 3.94 min, m/z 401 [MH+].

1. customwas irradiated in the microwave at 100° C. for 20 min
2. extractionextracted with EtOAc (×2)
3. washThe combined organics were washed with brine
4. dry with materialdried (MgSO4)
5. filtrationfiltered
6. customevaporated in vacuo
7. customThe residue was purified by FCC