反应详情

7-Chloro-3-(3-pyrazol-1-yl-phenyl)-imidazo[1,2-a]pyridine (Intermediate AA) (1 eq, 0.214 mmol, 70 mg) and 3-pyridine boronic acid (1 eq, 0.214 mmol, 26.1 mg) are dissolved in DME (3 ml), EtOH (1 ml) and water (1.5 ml) and Na2CO3 (2 eq, 0.427 mmol, 53.0 mg) is added. Pd(PPh3)4 (0.06 eq, 0.01 mmol, 15 mg) is added and the reaction mixture is heated using microwave radiation at 120° C. for 15 min. At the completion of this time the solvent is removed in vacuo and the reaction mixture is purified by flash column chromatography eluting with 8:2 DCM/MeOH to yield 3-(3-pyrazol-1-yl-phenyl)-7-pyridin-3-yl-imidazo[1,2-a]pyridine as a light brown solid; [M+H]+=338

1. temperaturethe reaction mixture is heated
2. customat 120° C.
3. customfor 15 min
4. customAt the completion of this time the solvent is removed in vacuo
5. customthe reaction mixture is purified by flash column chromatography
6. washeluting with 8:2 DCM/MeOH