State Key Laboratory of Natural and Biomimetic Drugs, Peking University, School of Pharmaceutical Sciences, Peking University, Xue Yuan Rd. 38, Beijing 100191, China.
Org Lett. 2012 Sep 21;14(18):4926-9. doi: 10.1021/ol302270z. Epub 2012 Sep 4.
A novel and efficient copper or nickel catalyzed highly selective denitrogenative annulation of vinyl azides with aryl acetaldehydes has been developed. 2,4- and 3,4-diaryl substituted pyrroles, which are difficult to synthesize by the reported methods, can be highly regioselectively prepared by this protocol simply switched by the selection of the transition metal catalysts. Compared with the reported acidic or basic conditions for polysubstituted pyrrole synthesis, the present reaction conditions are mild, neutral, and very simple without any additives.
一种新型高效的铜或镍催化的芳基乙醛与乙烯基叠氮化物的高选择性去氮环化反应已被开发出来。通过这种方案，可以简单地通过选择过渡金属催化剂来高度区域选择性地制备 2,4-和 3,4-二芳基取代的吡咯，这些吡咯用报道的方法很难合成。与报道的用于多取代吡咯合成的酸性或碱性条件相比，本反应条件温和、中性且非常简单，无需添加任何助剂。
