反应详情

温度

120 °C

A mixture of 5-chloro-1H-pyrrolo[3,2-b]pyridine (150 mg, 0.983 mmol, Matrix Scientific), 2-fluorophenylboronic acid (275 mg, 1.966 mmol, Aldrich) and dichloro 1,1′-bis(diphenylphosphino)ferrocene palladium (II) (80 mg, 0.098 mmol, Strem) was capped, degassed and backfilled with argon (3×). Toluene (2 mL), EtOH (2 mL) and Na2CO3, 2.0 M (0.983 mL, 1.966 mmol) were added, and the reaction was heated to 120° C. in a microwave for 45 min. The solution was diluted with EtOAc (50 mL) and washed with brine (50 mL), dried over MgSO4, concentrated in vacuo and purified by silica gel chromatography (eluent: 1-4% MeOH/DCM), affording 5-(2-fluorophenyl)-1H-pyrrolo[3,2-b]pyridine (200 mg, 96%). MS (ESI, pos. ion) m/z: 213.1 (M+1).

1. customwas capped
2. customdegassed
3. additionToluene (2 mL), EtOH (2 mL) and Na2CO3, 2.0 M (0.983 mL, 1.966 mmol) were added
4. additionThe solution was diluted with EtOAc (50 mL)
5. washwashed with brine (50 mL)
6. dry with materialdried over MgSO4
7. concentrationconcentrated in vacuo
8. custompurified by silica gel chromatography (eluent: 1-4% MeOH/DCM)