Triethylamine → 2-Amino-N-(5-benzyloxy-benzofuran-2-ylmethyl)-6-methoxymethyl-nicotinamide

Participants

Reaction Steps

To a N,N-dimethylformamide (5 mL) solution of C-(5-benzyloxy-benzofuran-2-yl)-methylamine (135 mg, 533 μmol) described in Production Example 7-1-6 were added 2-amino-6-methoxymethyl-nicotinic acid (107 mg, 586 μmol) described in Production Example 4-1-5, triethylamine (223 μL, 1.60 mmol) and benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (306 mg, 693 μmol) at room temperature, which was stirred at room temperature for 27 hours. Water was added to the reaction solution at room temperature followed by extracting with ethyl acetate. The organic layer was washed with water and sat. NaCl followed by drying over anhydrous magnesium sulfate and filtering. The filtrate was concentrated under a reduced pressure and the residue was purified by silica gel column chromatography (heptane:ethyl acetate=1:5) to obtain the title compound (166 mg, 75%) as a white solid.

Provenance & Evidence