反应详情

温度

170 °C

A mixture of 4-(5-chloro-furo[2,3-c]pyridin-2-yl)-piperidine-1-carboxylic acid tert-butyl ester (390 mg), 4-(methanesulfonyl)phenyl boronic acid (350 mg), 2 M aqueous Na2CO3 solution (1.50 mL), and 1,4-dioxane (10 mL) is sparged with Ar for 10 min. Pd(PPh3)4 (100 mg) is added and the resulting mixture is stirred at 170° C. for 1 h in a microwave oven. The reaction mixture is concentrated, diluted with water, and extracted with ethyl acetate. The combined extracts are washed with brine, dried (MgSO4), and concentrated. The residue is chromatographed on silica gel (cyclohexane/ethyl acetate 60:40→40:60) to give the title compound. LC (method 2): tR=1.23 min; Mass spectrum (ESI+): m/z=457 [M+H]+.

1. customis sparged with Ar for 10 min
2. additionPd(PPh3)4 (100 mg) is added
3. concentrationThe reaction mixture is concentrated
4. additiondiluted with water
5. extractionextracted with ethyl acetate
6. washThe combined extracts are washed with brine
7. dry with materialdried (MgSO4)
8. concentrationconcentrated
9. customThe residue is chromatographed on silica gel (cyclohexane/ethyl acetate 60:40→40:60)