反应详情

温度

85 °C

(S)-tert-Butyl 4-(1-cyano-2-(4-iodophenyl)ethylcarbamoyl)tetrahydro-2H-pyran-4-ylcarbamate (Example 15, step (i), 200 mg) and 4-carbamoyl-3-fluorophenylboronic acid (73 mg) in acetonitrile (8 mL) were treated with potassium acetate (79 mg) in water (4 mL). Nitrogen was bubbled through the mixture and then 1,1 bis(di-tert-butylphosphino)ferrocene palladium dichloride (5 mg) was added and the mixture was heated at 85° C. for 18 h under nitrogen. The reaction mixture was evaporated onto silica and purified by chromatography on silica eluting with ethyl acetate/isohexane (50:50 to 100:0) to afford the sub-titled compound (108 mg).

1. customNitrogen was bubbled through the mixture
2. addition1,1 bis(di-tert-butylphosphino)ferrocene palladium dichloride (5 mg) was added
3. customThe reaction mixture was evaporated onto silica
4. custompurified by chromatography on silica eluting with ethyl acetate/isohexane (50:50 to 100:0)