反应详情

温度

85 °C

(S)-tert-Butyl 4-(1-amino-1-oxo-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)propan-2-ylcarbamoyl)tetrahydro-2H-pyran-4-ylcarbamate (Example 16, step (i), 250 mg) in acetonitrile (8 mL) with 5-bromo-3-(2-methoxyethyl)benzo[d]oxazol-2(3H)-one (Example 24, step (i), 131 mg) was treated with an aqueous solution of sodium carbonate (2M, 0.483 mL). Nitrogen was bubbled through the solution and then 1,1 bis(di-tert-butylphosphino)ferrocene palladium dichloride (5 mg) was added. The reaction mixture was heated at 85° C. for 18 h under nitrogen and allowed to cool to room temperature. Purification by chromatography on silica eluting with 50-100% ethyl acetate/isohexane as eluent afford the sub-titled compound (66 mg).

1. customNitrogen was bubbled through the solution
2. addition1,1 bis(di-tert-butylphosphino)ferrocene palladium dichloride (5 mg) was added
3. temperatureto cool to room temperature
4. customPurification by chromatography on silica eluting with 50-100% ethyl acetate/isohexane as eluent