Department of Organic Chemistry University of Madras, Chennai-025, Tamilnadu, India.
Org Biomol Chem. 2020 Dec 21;18(47):9601-9605. doi: 10.1039/d0ob02234a. Epub 2020 Nov 23.
The use of the in situ generated ligand-copper superoxo complex absorbing light energy to activate the alpha C(sp)-H of MeOH and EtOH via the hydrogen atom transfer (HAT) process for the synthesis of quinazolinones by oxidative cyclization of alcohols with o-aminobenzamide has been investigated. The synthetic utility of this protocol offers an efficient synthesis of a quinazolinone intermediate for erlotinb (anti-cancer agent) and 30 examples were reported.
研究了通过原位生成的配体-铜过氧配合物吸收光能,通过氢原子转移(HAT)过程激活 MeOH 和 EtOH 的α C(sp)-H,实现醇与邻氨基苯甲酰胺的氧化环化合成喹唑啉酮。该方法的合成实用性为厄洛替尼(抗癌剂)的喹唑啉酮中间体提供了一种有效的合成方法,共报道了 30 个实例。