Tayu Masanori, Nomura Kazuya, Kawachi Koki, Higuchi Kazuhiro, Saito Nozomi, Kawasaki Tomomi
Meiji Pharmaceutical University, 2-522-1, Noshio, Kiyose, Tokyo, 204-8588, Japan.
Chemistry. 2017 Aug 10;23(45):10925-10930. doi: 10.1002/chem.201702338. Epub 2017 Jul 20.
An indole core bearing a functional group on the C2 position is often found as a key structure in biologically active natural products and pharmaceuticals. Here, we report direct C2-functionalization of indoles triggered by the formation of an iminium species generated from indole and a sulfonium reagent. The reaction proceeded under very mild conditions to give the corresponding C2-substituted indole derivatives in good to high yields.
在具有生物活性的天然产物和药物中，常常能发现吲哚核心在C2位带有一个官能团。在此，我们报道了由吲哚和锍试剂生成的亚胺离子物种引发的吲哚直接C2官能化反应。该反应在非常温和的条件下进行，能以良好至高的产率得到相应的C2-取代吲哚衍生物。
