苯并噁嗪酮及其衍生物具有重要的医用价值及生理活性,因此合成该类骨架结构受到很多化学家的重视.报道了一种以含N,O-双齿导向基团的苯氧乙酸为底物,通过钯催化的C—H键活化反应一步构建C—N键的新方法,合成了一系列苯并噁嗪类化合物.该方法反应条件温和,操作简便,合成效率高.
Benzoxazinone and its derivatives are well-known as a broad-spectrum of physiological activities compounds. Herein we report a novel approach for the synthesis of benzoxazine derivatives via a N,O-bindentate directing assisted Pd-catalyzed intramolecular amination reactions. Various benzoxazinone derivatives are obtained in moderate to good yields. The directing group can be removed under mild condition, highlighting potential synthetic utility of this method.