Triethylamine → 2-Amino-N-(6-benzyloxy-benzofuran-2-ylmethyl)-6-methoxymethyl-nicotinamide

Participants

Reaction Steps

To a N,N-dimethylformamide (8 mL) solution of C-(6-benzyloxy-benzofuran-2-yl)-methylamine (400 mg, 1.58 mmol) described in Production Example 1-2-4 were added 2-amino-6-methoxymethyl-nicotinic acid (316 mg, 1.74 mmol) described in Production Example 4-1-5, triethylamine (660 μL, 4.74 mmol) and benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (908 mg, 2.05 mmol) at room temperature, which was stirred at room temperature for 2 hours 30 minutes. To the reaction solution was added water at room temperature followed by extraction with ethyl acetate. After washing the organic layer with water and sat. NaCl, the organic layer was dried over anhydrous magnesium sulfate and filtered. The filtrate was concentrated under a reduced pressure and purified by silica gel column chromatography (heptane:ethyl acetate=1:2) to obtain the title compound (454 mg, 69%) as a white solid.

Provenance & Evidence