The Institute of Next Generation Matter Transformation, College of Chemical Engineering & College of Material Sciences Engineering, Huaqiao University , 668 Jimei Blvd., Xiamen, Fujian 361021, PR China.
Org Lett. 2017 Sep 15;19(18):4726-4729. doi: 10.1021/acs.orglett.7b02015. Epub 2017 Aug 29.
A highly efficient synthesis of 3-formyl imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrimidine, under Cu-catalyzed aerobic oxidative conditions and by utilizing ethyl tertiary amines as carbon sources, is disclosed. A novel activation mode of ethyl tertiary amines in which simultaneous selective cleavage of C-C bond and C-N bond of ethyl group with molecular oxygen as terminal oxidant in this one-pot protocol is reported for the first time. This reaction features broad substrate scope, good functional group tolerance, as well as diversified and valuable products.
本文报道了一种在铜催化有氧氧化条件下，利用叔乙基胺作为碳源高效合成 3-甲酰基咪唑并[1,2-a]吡啶和咪唑并[1,2-a]嘧啶的方法。该一锅法反应中，叔乙基胺的 C-C 键和 C-N 键被同时选择性切断，分子氧作为末端氧化剂，这是叔乙基胺的一种新的活化模式。该反应具有广泛的底物范围、良好的官能团耐受性以及多样化和有价值的产物。
