5-(Methylsulphonyl)pyridine-3-boronic acid → 4-Fluoro-1-(2-fluoro-5-(5-(methylsulfonyl)pyridin-3-yl)phenyl)-1-(2-methylpyridin-4-yl)-1H-isoindol-3-amine

Participants

Reaction Steps

The title compound was synthesized as described for Example 1 in 32% yield, starting from 1-(5-bromo-2-fluorophenyl)-4-fluoro-1-(2-methylpyridin-4-yl)-1H-isoindol-3-amine (80 mg, 0.19 mmol) and 5-(methylsulfonyl)pyridin-3-ylboronic acid (50.5 mg, 0.25 mmol). 1H NMR (500 MHz, DMSO-d6, 298 K) δ ppm 9.07 (d, 1 H), 9.04 (d, 1 H), 8.39 (t, 1 H), 8.31 (d, 1 H), 7.84 (m, 1 H), 7.62-7.69 (m, 2 H), 7.56 (m, 1 H), 7.38 (dd, 1 H), 7.28-7.34 (m, 1 H), 7.04 (s, 1 H), 6.98 (dd, 1 H), 6.76 (br. s., 2 H), 3.37 (s, 3 H), 2.38 (s, 3 H); MS (ES+) m/z 491 (M+1).

Provenance & Evidence