4-Fluoro-3-(pyridin-3-yl)benzeneboronic acid → 2-[3-(4-Fluoro-3-(pyridin-3-yl)phenyl)imidazo[1,2-alpha]pyrimidin-7-yl]-2-methylpropan-1-ol

Participants

Reaction Steps

3-Bromo-7-(1,1-dimethyl-2-triethylsilanyloxyethyl)imidazo[1,2-α]pyrimidine was coupled to 4-fluoro-3-(pyridin-3-yl)benzeneboronic acid (323 mg, 1.28 mmol) following the procedure in Example 65 and deprotected as described in Example 8 to give 2-[3-(4-fluoro-3-(pyridin-3-yl)phenyl)imidazo[1,2-α]pyrimidin-7-yl]-2-methylpropan-1-ol as a white powder: δH (360 MHz, CDCl3) 1.39 (6H, s), 3.54 (1H, t, J 7), 3.89 (1H, d, J 7), 6.99 (1H, d, J 7), 7.35-7.45 (2H, m), 7.51-7.60 (2H, m), 7.83 (1H, s), 7.90-7.94 (1H, m), 8.53 (1H, d, J 7), 8.68 (1H, dd, J 5 and 2), 8.83 (1H, s); m/z (ES+) 363 (M++H).

Provenance & Evidence