反应详情

温度

135 °C

To a 1-methyl-2-pyrrolidinone (500 μL) solution of trifluoromethanesulfonic acid 2-(((2-amino-6-methoxymethyl-pyridin-3-carbonyl)-amino)-methyl)-benzofuran-6-yl ester (15 mg, 33 μmol) described in Production Example 47-1 were added tributyl-methoxymethyl-stannane (14 mg, 43 μmol), tetrakis(triphenylphosphine)palladium (0) (3.78 mg, 3.3 μmol) and tetrabutyl ammonium chloride (1.82 mg, 6.5 μmol) at room temperature, which was stirred at 135° C. for 4 hours under nitrogen atmosphere. After allowing the reaction solution to cool to room temperature, the reaction solution was filtered and purified by reverse phase high-performance liquid chromatography (using an acetonitrile-aqueous mobile phase (containing 0.1% trifluoroacetic acid)) followed by further purifying by silica gel column chromatography (ethyl acetate) to obtain the title compound (0.7 mg, 6%) as a white solid.

1. temperatureto cool to room temperature
2. filtrationthe reaction solution was filtered
3. custompurified by reverse phase high-performance liquid chromatography (
4. additionan acetonitrile-aqueous mobile phase (containing 0.1% trifluoroacetic acid))
5. customby further purifying by silica gel column chromatography (ethyl acetate)