反应详情

温度

85 °C

(S)-tert-Butyl 4-(1-amino-3-(4-iodophenyl)-1-oxopropan-2-ylcarbamoyl)tetrahydro-2H-pyran-4-ylcarbamate (Example 1, step (iii), 300 mg) and 3-(methylsulfonyl)phenylboronic acid (122 mg) in acetonitrile (8 mL) were treated with an aqueous solution of sodium carbonate (2M, 0.58 mL) and nitrogen was bubbled through the mixture. 1,1 bis(Di-tert-butylphosphino)ferrocene palladium dichloride (5 mg) was added and the reaction mixture was heated at 85° C. for 18 h. The mixture was purified by chromatography on silica eluting with 50-100% ethyl acetate/isohexane as eluent to yield the sub-titled compound (320 mg).

1. customwas bubbled through the mixture
2. addition1,1 bis(Di-tert-butylphosphino)ferrocene palladium dichloride (5 mg) was added
3. customThe mixture was purified by chromatography on silica eluting with 50-100% ethyl acetate/isohexane as eluent