(2-Methanesulfonylphenyl)methanamine → 5-bromo-8-hydroxy-N-[2-(methylsulfonyl)benzyl]-1,6-naphthyridine-7-carboxamide

Participants

Reaction Steps

Methyl 5-bromo-8-hydroxy-1,6-naphthyridine-7-carboxylate (500 mg, 1.77 mmol, prepared as in Example 113) and 1-[2-(methylsulfonyl)phenyl]methanamine (491 mg, 2.65 mmol) were suspended in 10 mL methanol in an oven-dried Schlenck tube. The solution was purged with Argon for 1 minute and capped. The solution was heated to 80 deg C. with stirring over 4 days. Upon cooling a white solid precipitated out of the methanol. LCMS analysis indicated that the precipitate was the desired product. Filtration and subsequent washing with methanol (10 mL) afforded the desired material as a white solid.

Provenance & Evidence