反应详情

温度

75 °C

(S)-tert-Butyl 4-(1-amino-3-(4-iodophenyl)-1-oxopropan-2-ylcarbamoyl)tetrahydro-2H-pyran-4-ylcarbamate (Example 1, step (iii), 346 mg) in acetonitrile (10 mL) under nitrogen was treated with 3-cyano-4-fluorophenylboronic acid (110 mg) followed by aqueous potassium carbonate solution (2M, 0.67 mL) and 1,1 bis(di-tert-butylphosphino)ferrocene palladium dichloride (9 mg). The mixture was stirred at 75° C. for 18 h. The reaction mixture was evaporated, dissolved in dichloromethane, absorbed onto silica and purified by chromatography on silica eluting with 50% ethyl acetate in isohexane, then 100% ethyl acetate to afford the titled compound (366 mg).

1. customThe reaction mixture was evaporated
2. dissolutiondissolved in dichloromethane
3. customabsorbed onto silica
4. custompurified by chromatography on silica eluting with 50% ethyl acetate in isohexane