反应详情

A microwave vial is charged with pyridine-3-boronic acid (0.031 g, 0.25 mmol), 2M aqueous sodium carbonate (1 ml) and DME (3 ml) and then purged with Argon for 30 minutes at room temperature. 1-(6-Bromo-imidazo[1,2-a]pyridin-2-yl)-3-[2-(2-isopropyl-2H-tetrazol-5-yl)-ethyl]-urea (Intermediate E1)(0.05 g, 0.13 mmol) and [1,1′-Bis(diphenylphosphino)ferrocene]palladium(II) chloride (0.016 g, 0.02 mmol) are added and the reaction mixture is heated using microwave radiation at 100° C. for 30 minutes. The reaction mixture is filtered through Celite® (filter agent) and washed through with EtOAc. The crude product is absorbed on silica and purified by flash chromatography, eluting with methanol in DCM (3%) to afford the title compound.

1. custompurged with Argon for 30 minutes at room temperature
2. temperaturethe reaction mixture is heated
3. customat 100° C.
4. customfor 30 minutes
5. filtrationThe reaction mixture is filtered through Celite® (filter agent)
6. washwashed through with EtOAc
7. customThe crude product is absorbed on silica
8. custompurified by flash chromatography
9. washeluting with methanol in DCM (3%)