反应详情

Heat a mixture of Pd(OAc)2 (1.25 g, 5.59 mmol), CuI (0.42 g, 2.23 mmol), P(t-Bu)3 (2.76 mL, 11.2 mmol), K2CO3 (30.3 g, 223.8 mmol) and 6-bromo-1-isobutyl-1H-benzimidazol-2-ylamine (30 g, 111.9 mmol) in DMSO (200 mL) at 70° C. Add phenylacetylene (14.6 mL, 133.4 mmol) and heat the mixture for 6 hours at 70° C. Cool and dilute with H20. Filter the residue through a pad of celite. Recrystallize the crude mixture in toluene to give the desired compound as a white solid (19.68 g, 60%).

1. temperatureHeat
2. temperatureCool
3. additiondilute with H20
4. filtrationFilter the residue through a pad of celite
5. customRecrystallize the crude mixture in toluene