反应详情

温度

110 °C

5-Bromo-6-methyl-pyridine-2-carbonitrile (0.5 g, 2.5 mmol), cyclopropylboronic acid (CAN:411235-57-9, 0.36 g, 4 mmol), Pd2(dba)3 (CAN:411235-57-9, 0.1 g, 0.2 mmol), xantphos (CAN:161265-03-8, 0.15 g, 0.26 mmol) and Cs2CO3 (1.1 g, 3 mmol) were suspended in 1,4-dioxane (30 mL) under a nitrogen atmosphere. The mixture was stirred for 12 h at 110° C., filtered, concentrated under reduced pressure and purified by column chromatography (silica gel, 5 g, eluting with 10% ethyl acetate in petroleum ether) to give the title compound (0.3 g, 75%) as yellow solid; MS (D): m/e=159.2 [M+H]+.

1. filtrationfiltered
2. concentrationconcentrated under reduced pressure
3. custompurified by column chromatography (silica gel, 5 g, eluting with 10% ethyl acetate in petroleum ether)