2-羟基喹啉合成新方法研究

A New Synthetic Method of 2-Quinolinones

本研究利用简单的乙酰苯胺和丙烯酸酯作为起始原料,在过硫酸钾做氧化剂,水合对甲苯磺酸做添加剂的条件下,通过钯催化的C-H键活化/C-C键生成/环化串联反应以46%~95%收率合成了一系列2-羟基喹啉衍生物.本研究为2-羟基喹啉衍生物的合成提供了实用的合成方法.

A series of 2-bydroxyquinoline derivatives were synthesized in 46%- 95% yields via a C-H bond activation/C- C bond formation/cyclization cascade process with simple acetanilides and ethyl acrylates as the substrates by using Pd（OAc）2 as catalyst, K2 S2O8 as oxidant and TsOH·H2O as additive. This finding provides a practical procedure for the synthesis of 2- hydroxyquinoline derivatives. Keywords： 2-quinolinone, palladium acetate, C-H activation.