反应详情

温度

90 °C

(2S)-2-[(5-bromopyridin-2-yl)(phenyl)methoxy]-N-(cyanomethyl)-4-methylpentanamide from example 53 step 3 (156 mg, 0.375 mmol), 4-piperazine-1-ylphenyl boronic acid (100 mg, 0.413 mmol, 1.1 eg), [1,1′-Bis(diphenylphosphino)-ferrocene dichloropalladium II complex with CH2Cl2 (13.7 mg, 0.0187 mmol, 0.05 eg), sodium carbonate (2M soln, 750 uL, 1.5 mmol, 4 eg) were mixed together in DMF (5 mL). The reaction mixture was degased 3× with N2, then heated to 90° C. for 5 hours. After cooling, the mixture was evaporated under high vacuum and residue was chromatographed with a mixture of dichloromethane/methanol/ammonium hydroxide (90:9:1) to give the title compound.

1. customThe reaction mixture was degased 3× with N2
2. temperatureAfter cooling
3. customthe mixture was evaporated under high vacuum and residue
4. customwas chromatographed with a mixture of dichloromethane/methanol/ammonium hydroxide (90:9:1)