College of Pharmaceutical Engineering of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, P. R. China.
Org Biomol Chem. 2021 Jun 28;19(24):5377-5382. doi: 10.1039/d1ob00731a. Epub 2021 May 28.
Described here is a general and highly efficient method for the synthesis of 1H- and 3H-indoles. In the presence of CBr and a suitable base, the cyclization of N-aryl enamines proceeds with high efficiency. Unlike previous intramolecular cross dehydrogenative coupling (CDC) of the same substrates, this process does not require the use of either a transition metal or a stoichiometric amount of oxidant. This method also features operational simplicity, easy scalability and good substrate tolerability. Control experiments indicate the reactions may proceed in a tandem sequence of bromination and intramolecular Friedel-Crafts alkylation in a simple one-pot procedure.
这里描述了一种通用且高效的合成 1H-和 3H-吲哚的方法。在 CBr 和合适的碱存在下，N-芳基烯胺的环化反应具有很高的效率。与以前相同底物的分子内交叉脱氢偶联（CDC）不同，该过程不需要使用过渡金属或化学计量的氧化剂。该方法还具有操作简单、易于规模化和良好的底物耐受性等特点。控制实验表明，反应可能在一个简单的一锅法中通过溴化和分子内傅克烷基化的串联序列进行。
