5-chloro-2-(trifluoromethyl)-1,8-Naphthyridine → 5-(2-Fluoro-3-pyridin-4-ylphenyl)-2-trifluoromethyl[1,8]naphthyridine

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Reaction Steps

5-Chloro-2-trifluoromethyl[1,8]naphthyridine (50 mg, 0.22 mmol) was coupled to 2-fluoro-3-(pyridin-4-yl)benzeneboronic acid (61 mg, 0.28 mmol) as described in Example 7 part g), affording 5-(2-fluoro-3-pyridin-4-ylphenyl)-2-trifluoromethyl[1,8]naphthyridine (37 mg, 47%). δH (360 MHz, CDCl3) 7.45-7.54 (4H, m), 7.65 (1H, d, J 4.2), 7.68-7.74 (1H, m), 7.84 (1H, d, J 8.4), 8.35 (1H, dd, J 2.5 and 8.8), 8.72-8.74 (2H, m), 9.34 (1H, d, J 4.2). m/z (ES+) 370 [MH]+.

Provenance & Evidence