反应详情

温度

100 °C

A suspension of methyl 2-(4-chloro-6-methyl-2-(piperidin-1-yl)pyrimidin-5-yl)pentanoate (0.081 g; 0.25 mmol), tetrakis(triphenylphosphine) palladium(0) (0.029 g; 0.025 mmol), N,N-diisopropylethylamine (0.172 mL; 1.00 mmol) and 2-chloro-4-methylphenylboronic acid (0.064 g; 0.375 mmol) in a mixture of DME-water (3:1, 1 mL) was heated at 100° C. in a sealed tube for 2.5 h. The mixture was diluted with brine and extracted with ethyl acetate. The combined organics were dried over magnesium sulphate, filtered and concentrated under reduced pressure. Purification by flash-chromatography on silica gel using a gradient of methanol (1-10%) in dichloromethane furnished 0.069 g (64%) of the title compound as a colorless oil.

1. extractionextracted with ethyl acetate
2. dry with materialThe combined organics were dried over magnesium sulphate
3. filtrationfiltered
4. concentrationconcentrated under reduced pressure
5. customPurification by flash-chromatography on silica gel using a gradient of methanol (1-10%) in dichloromethane