State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry , Nankai University , Tianjin 300071 , People's Republic of China.
Collaborative Innovation Center of Chemical Science and Engineering (Tianjin) , Tianjin 300071 , People's Republic of China.
J Org Chem. 2018 Apr 20;83(8):4516-4524. doi: 10.1021/acs.joc.8b00235. Epub 2018 Mar 30.
We report a protocol for the synthesis of N, N- and N, O-aminals via direct azidation of sp C-H bonds of substrates with an α-nitrogen or α-oxygen atom. A broad range of tetrahydroisoquinolines, tetrahydro-β-carbolines, and cyclic benzyl ethers gave high yields under mild conditions. The protocol could be carried out on a gram scale without a decrease in the yield, and the aminal products could be readily transformed into complex aminals.
我们报告了一种通过直接氮原子或氧原子α位的 sp³ C-H 键的氮丙啶化反应来合成 N,N-和 N,O-缩胺的方法。该方法在温和条件下可以高产率得到一系列四氢异喹啉、四氢-β-咔啉和环状苄基醚类化合物。该反应可以克级规模进行，且产率没有降低，缩胺产物可以很容易地转化为复杂的缩胺。
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