反应详情

温度

130 °C

2-Amino-6-chloro-N-(5-phenoxy-thiophen-2-ylmethyl)-nicotinamide described in Example A-101 (20 mg, 37 μmol) and 2-pyridin-2-yl-ethyl amine (66 μl, 0.56 mmol) were dissolved in a mixture solvent of dimethylsulfoxide (1 mL) and N,N-diisopropylethylamine (0.5 mL), and the solution was stirred at 130° C. for 17 hours. The reaction solution was cooled to room temperature, water and ethyl acetate were added, the organic layer was partitioned, washed with water and brine, and dried over anhydrous magnesium sulfate. The solvent was evaporated in vacuo, the residue was purified by reverse phase high performance liquid chromatography (acetonitrile-water mobile phase (containing 0.1% trifluoroacetic acid) was used), and the title compound (17.7 mg) was obtained as a trifluoroacetic acid salt.

1. temperatureThe reaction solution was cooled to room temperature
2. customthe organic layer was partitioned
3. washwashed with water and brine
4. dry with materialdried over anhydrous magnesium sulfate
5. customThe solvent was evaporated in vacuo
6. customthe residue was purified by reverse phase high performance liquid chromatography (acetonitrile-water mobile phase (containing 0.1% trifluoroacetic acid) was used)