反应详情

A solution of 2-amino-nicotinic acid (21 mg, 0.15 mmol), C-(5-(4-chloro-phenoxy)-thiophen-2-yl)-methylamine described in Preparation Example 157 (36 mg, 0.15 mmol), benzotriazol-1-yl-tris(dimethylamino)phosphonium hexafluorophosphate (86 mg, 0.195 mmol) and triethylamine (0.065 mL, 0.45 mmol) in dimethylsulfoxide (1 mL) was stirred under nitrogen atmosphere for 17 hours at room temperature. This reaction solution was purified by reverse phase high performance liquid chromatography (acetonitrile-water mobile phase (containing 0.1% trifluoroacetic acid) was used), and trifluoroacetic acid salt of the title compound (17.7 mg, 0.037 mmol, 24.9%) was obtained as a pale yellow solid.