Feng Enguang, Huang He, Zhou Yu, Ye Deju, Jiang Hualiang, Liu Hong
The Center for Drug Discovery and Design, State Key Laboratory of Drug Research, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, 201203, China.
J Org Chem. 2009 Apr 3;74(7):2846-9. doi: 10.1021/jo802818s.
We developed an efficient and convenient method for preparing N-substituted 2H-1,4-benzoxazin-3-(4H)-ones from 2-halophenols via a nucleophilic substitution with 2-chloroacetamides followed by a CuI-catalyzed coupling cyclization. A broad spectrum of substrates can be effectively employed to afford the desired products in good yields. Since this method involves simple reaction conditions, a short reaction time, and a broad substrate scope, it is particularly attractive for the efficient preparation of biologically and medicinally interesting molecules.
我们开发了一种高效便捷的方法，可通过2-卤代苯酚与2-氯乙酰胺的亲核取代反应，随后进行碘化亚铜催化的偶联环化反应，从2-卤代苯酚制备N-取代的2H-1,4-苯并恶嗪-3-(4H)-酮。多种底物可有效用于以良好产率得到所需产物。由于该方法反应条件简单、反应时间短且底物范围广，对于高效制备具有生物学和医学意义的有趣分子特别有吸引力。
