3-(2-Fluoro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-YL)phenyl)pyridine → 7-(1-Fluoro-1-methylethyl)-3-[4-fluoro-3-(pyridin-3-yl)phenyl]imidazo[1,2-alpha]pyrimidine

Participants

Reaction Steps

3-Bromo-7-(1-fluoro-1-methylethyl)imidazo[1,2-α]pyrimidine was coupled with 3-[2-fluoro-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)phenyl]pyridine as described in Example 65 to afford 7-(1-fluoro-1-methylethyl)-3-[4-fluoro-3-(pyridin-3-yl)phenyl]imidazo[1,2-α]pyrimidine as a white solid after crystallisation from ethyl acetate/isohexane: δH (360 MHz, CDCl3) 1.74 (6H, d, J 22), 7.26 (1H, dd, J 7 and 2), 7.53-7.60 (2H, m), 7.80 (1H, ddd, J 8, 5 and 2), 7.94 (1H, dd, J 8 and 2), 8.05 (1H, s), 8.10 (1H, ddd, J 8, 4 and 2), 8.65 (1H, dd, J 5 and 1.5), 8.89 (1H, s), 9.13 (1H, d, J 7); m/z (ES+) 351 (M++H).

Provenance & Evidence