反应详情

1-(3-Bromophenyl)-1-(3-chloro-4-methoxyphenyl)-4-fluoro-1H-isoindol-3-amine (570 mg, 1.28 mmol), pyrimidin-5-ylboronic acid (190 mg, 1.53 mmol), cesium carbonate (1250 mg, 3.84 mmol) and dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium (II) dichloromethane adduct (104 mg, 0.13 mmol) were dissolved in DME:EtOH:Water (6:3:1) (5 mL) and irradiated in a microwave oven for 20 min at 150° C. EtOAc, water and brine were added. The organic phase was collected, dried, filtered and then the solvent was removed under reduced pressure. The residue was purified by preparative HPLC to give 212 mg (37%) of the title product. MS (ES+) m/z 445 [M+1]+.

1. customirradiated in a microwave oven for 20 min at 150° C
2. customThe organic phase was collected
3. customdried
4. filtrationfiltered
5. customthe solvent was removed under reduced pressure
6. customThe residue was purified by preparative HPLC