反应详情

300 mg (0.84 mmol) 9-Bromo-2-chloro-3-phenylpyrimido[1,2-b]indazole, (intermediate example Int-1-2), 128.7 mg (0.92 mmol) (4-fluorophenyl)boronic acid, 68.3 mg (0.084 mmol) bis(diphenylphosphino)ferrocenedichloropalladium(II) and 1.5 mL aqueous sodium carbonate solution (10%) in 10 mL dimethoxyethane were heated in the microwave oven for 45′ at 110° C. The reaction mixture was poured on water/dichloromethane and stirred vigorously for 30′. The organic phase was separated and washed twice with brine. After drying and filtration the solvent was evaporated and the residue (194 mg), a mixture (according to UPLC/MS) of the title compound, the regioisomer 9-bromo-2-(4-fluorophenyl)-3-phenyl-pyrimido[1,2-b]indazole and the bisproduct 2,9-bis-(4-fluorophenyl)-3-phenyl-pyrimido[1,2-b]indazole, was used in the next step without further purification.

1. customat 110° C
2. additionThe reaction mixture was poured on water/dichloromethane
3. customThe organic phase was separated
4. washwashed twice with brine
5. customAfter drying
6. filtrationfiltration the solvent
7. customwas evaporated
8. customthe residue (194 mg), a mixture (according to UPLC/MS) of the title compound, the regioisomer 9-bromo-2-(4-fluorophenyl)-3-phenyl-pyrimido[1,2-b]indazole and the bisproduct 2,9-bis-(4-fluorophenyl)-3-phenyl-pyrimido[1,2-b]indazole, was used in the next step without further purification