Transition-metal-free regioselective thiocyanation of phenols, anilines and heterocycles
Transition-metal-free regioselective thiocyanation of phenols, anilines and heterocycles
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DOI：
10.1016/j.tetlet.2016.12.043
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发表时间：
2017-02-01
影响因子：
1.8
通讯作者：
Bhat, Ramakrishna G.
中科院分区：
文献类型：
--
作者：
Mete, Trimbak B.;Khopade, Tushar M.;Bhat, Ramakrishna G.
介绍了一种直接和区域选择性硫氰化苯酚、苯胺和杂环的方法。在室温下无过渡金属的条件下，通过直接碳氢官能化实现转化，收率高。结果表明，该方法具有单选择性，多种官能团对反应条件耐受。该方案的实用性在PPAR三角洲激动剂前驱体的克级合成中得到了证明，收率很高。(C) 2016 Elsevier Ltd.版权所有。
An expedient direct and regioselective thiocyanation of phenols, anilines and heterocycles is described. Transformation is realized via the direct C-H functionalization under transition metal free conditions at ambient temperature in excellent yields. Method proved to be monoselective and variety of functional groups tolerated the reaction conditions. The practicality of the protocol is demonstrated in gram scale synthesis of a precursor of PPAR delta agonist in excellent yield. (C) 2016 Elsevier Ltd. All rights reserved.