反应详情

温度

100 °C

3-Quinoline boronic acid (2.42 mmol, 420 mg), K3PO4 (3.63 mmol, 771 mg), and PdCl2(dppf).CH2Cl2 (0.121 mmol, 100 mg) was added to a solution of 4-{7-[Bis-(2-trimethylsilanyl-ethoxymethyl)-amino]-3-iodo-pyrazolo[1,5-a]pyrimidin-5-yl}-cyclohexanecarboxylic acid methyl ester (1.21 mmol, 800 mg) in dioxane (10 mL). To this suspension was added distilled H2O (1.0 mL). The resulting reaction mixture was stirred at 100° C. under an argon atmosphere for 18 hours. The reaction mixture was concentrated in vacuo and then purified via silica gel chromatography (0% to 60% ethyl acetate in hexanes gradient) to yield the title compound (630 mg, 79% yield) as yellow oil. LC-MS: 662 [M+H].

1. additionTo this suspension was added
2. distillationdistilled H2O (1.0 mL)
3. customThe resulting reaction mixture
4. concentrationThe reaction mixture was concentrated in vacuo
5. custompurified via silica gel chromatography (0% to 60% ethyl acetate in hexanes gradient)