反应详情

温度

100 °C

A mixture of Example 18A (1.0 equivalents), cyclopropyl boronic acid (1.1 equivalents), tricyclohexylphosphine (0.05 equivalents), palladium acetate (0.025 equivalents) and K3PO4 (2 equivalents) in a 20:1 volume ratio of toluene and water was sparged with nitrogen for 15 minutes. The reaction mixture was then heated to 100° C. for 12 hours, cooled, diluted with water, stirred for 1 hour and filtered through a diatomaceous earth pad, and the pad was rinsed with toluene. The filtrate was mixed and the layers were separated. The organic layer was washed with water and saturated brine, dried (Na2SO4), filtered and concentrated to an oil that was used without further purification.

1. temperaturecooled
2. filtrationfiltered through a diatomaceous earth pad
3. washthe pad was rinsed with toluene
4. additionThe filtrate was mixed
5. customthe layers were separated
6. washThe organic layer was washed with water and saturated brine
7. dry with materialdried (Na2SO4)
8. filtrationfiltered
9. concentrationconcentrated to an oil that
10. customwas used without further purification