A new general approach to 4-substituted-3-halo-2-quinolones

作者：Zhao Shuai; He Yan hong; Wu Di; Guan Zhi^*

来源：Journal of Fluorine Chemistry, 2010, 131(5): 597-605.

DOI：10.1016/j.jfluchem.2010.01.008

• 2-Quinolones
• 4-Substituted-3-fluoro-2-quinolones
• 4-Substituted-3-chloro-2-quinolones
• 4-Substituted-3-bromo-2-quinolones
• Horner-Wadsworth-Emmons olefination

A general procedure for the preparation of 4-substituted-3-halo-2-quinolones (halo = F, Cl, Br) utilizing 2-halo diethylphosphonoacetic acids (halo = F, Cl, Br) and o-aminophenylketones as the starting materials is described. The title compounds are obtained by an intramolecular Homer-Wadsworth-Emmons olefination of halogen-containing N-acyl-o-aminophenylketones. The transformation process is generally applicable under mild conditions.

• 出版日期2010-5
• 单位西南大学