Department of Chemistry, Northeast Normal University, Changchun, 130024, PR China.
J Org Chem. 2012 Jun 1;77(11):5173-8. doi: 10.1021/jo300615t. Epub 2012 May 11.
A new benzannulation strategy that proceeds via a regiospecific [4 + 2] cycloaddition of readily available cyclobutenones and active methylene ketones has been developed. On the basis of this strategy, persubstituted phenols/anilines with up to six different functional groups on the benzene ring were synthesized in a single step. In addition, a series of acridine derivatives were prepared in excellent yield from persubstituted phenols/anilines.
一种新的苯并环化策略已经被开发出来，该策略通过易于获得的环丁烯酮和活性亚甲基酮的区域特异性[4 + 2]环加成反应进行。在此策略的基础上，通过一步反应合成了苯环上带有多达六个不同官能团的取代苯酚/苯胺。此外，还从取代苯酚/苯胺中以优异的产率制备了一系列吖啶衍生物。
