反应详情

4-Iodo-3-propyl-1H-isochromen-1-one (intermediate C20.2, 0.80 g, 2.55 mmol), phenylboronic acid (0.39 g, 3.18 mmol), Pd(PPh3)4 (0.15 g, 0.127 mmol) and Cs2CO3 (1.16 g, 3.57 mmol) were reacted in DMF (10 ml) at 80° C. for 3 hrs. The reaction was the partitioned between AcOEt and 1 M HClaqueous, washed with 1 M HClaqueous brine, dried over Na2SO4 and concentrated under reduced pressure. The resulting crude was purified on a silica 500 Biotage cartridge eluting with a gradient of Hexane and AcOEt to give the title compound (0.11 g, 15.9%) as a yellowish oil.

1. custompartitioned between AcOEt and 1 M HClaqueous
2. washwashed with 1 M HClaqueous brine
3. dry with materialdried over Na2SO4
4. concentrationconcentrated under reduced pressure
5. customThe resulting crude was purified on a silica 500 Biotage cartridge
6. washeluting with a gradient of Hexane and AcOEt