2,4-Difluoro-3-(pyridin-3-yl)benzeneboronic acid → 5-(2,4-Difluoro-3-pyridin-3-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 2,4-difluoro-3-(pyridin-3-yl)benzeneboronic acid (66 mg, 0.28 mmol) as described in Example 7 part g), affording 5-(2,4-difluoro-3-pyridin-3-ylphenyl)-2-trifluoromethyl[1,8]naphthyridine (27 mg, 34%). δH (360 MHz, CDCl3) 7.28 (1H, m), 7.42-7.49 (2H, m), 7.63 (1H, d, J 4.6), 7.84-7.88 (2H, m), 8.35 (1H, dd, J 2.3 and 8.6), 8.69 (1H, dd, J 1.8 and 4.9), 8.80 (1H, s), 9.33 (1H, d, J 4.2). m/z (ES+) 388 [MH]+.

Provenance & Evidence