反应详情

To solution of 4-bromobenzonitrile (182 mg, 1.0 mmol) in 5 mL of dry THF at −78° C. was added n-BuLi (0.7 mL of 1.6 M hexanes solution, 1.1 mmol). The reaction was stirred 30 min and then 1-(4-fluorophenyl)-1H-indazol-5-carboxaldehyde (240 mg, 1.0 mmol) was added and the reaction mixture was allowed to warm to RT. After 12 h, quenched with brine and extracted 2×EtOAc. The organic layers were dried over MgSO4, filtered, and concentrated. The residue was purified on SiO2 by MPLC eluting with a 0-30% EtOAc/hexane gradient to give 180 mg (52% yield) of 4-((1-(4-fluorophenyl)-1H-indazol-5-yl)(hydroxy)methyl)benzonitrile. MS found: (M+H)+=344.

1. waitAfter 12 h
2. customquenched with brine
3. extractionextracted 2×EtOAc
4. dry with materialThe organic layers were dried over MgSO4
5. filtrationfiltered
6. concentrationconcentrated
7. customThe residue was purified on SiO2 by MPLC
8. washeluting with a 0-30% EtOAc/hexane gradient