3-bromo-7-(trifluoromethyl)imidazo[1,2-a]pyrimidine → 3-[4-Fluoro-3-([1,2,4]triazol-1-yl)phenyl]-7-trifluoromethylimidazo[1,2-alpha]pyrimidine

関与物質

反応手順

4-Fluoro-3-([1,2,4]triazol-1-yl)phenylboronic acid (100 mg, 0.48 mmol) was coupled to 3-bromo-7-trifluoromethylimidazo[1,2-α]pyrimidine (117 mg, 0.44 mmol) using the method in Example 1. Purification by chromatography on silica gel eluting with dichloromethane containing 2% methanol, then recrystallisation from dichloromethane/isohexane, gave 3-[4-fluoro-3-([1,2,4]triazol-1-yl)phenyl]-7-trifluoromethylimidazo[1,2-α]pyrimidine as a yellow solid: δH (360 MHz, CDCl3) 7.31 (1H, d, J 7), 7.51-7.60 (2H, m), 8.16 (2H, m), 8.21 (1H, dd, J 7 and 2), 8.80-8.83 (2H, m); m/z (ES+) 349 (M++H).

情報源と証拠