反应详情

温度

80 °C

To a microwave reactor tube was added 2-bromo-isonicotinic acid methyl ester (150 mg, 0.69 mmol), 1,3,5-trimethyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazole (197 mg, 0.83 mmol) and Pd2(PtBu3)2(14 mg, 0.028 mmol) and 1,4-dioxane (2 mL). The mixture was degassed and then 2M aqueous K3PO4 (0.46 mL, 1.4 mmol) was added. The mixture was heated in a microwave reactor at 80° C. for 1 hour. The cooled mixture was partitioned between CHCl3 and water. The organic layer was isolated and the product purified by SiO2 chromatography (0-15% MeOH in EtOAc) to give 2-(1,3,5-trimethyl-1H-pyrazol-4-yl-isonicotinic acid methyl ester (68 mg, 21%) as a yellow gum. MS(ESI) m/z 246 [M+H]+.

1. customThe mixture was degassed
2. customThe cooled mixture was partitioned between CHCl3 and water
3. customThe organic layer was isolated
4. customthe product purified by SiO2 chromatography (0-15% MeOH in EtOAc)