Regioselective acceptorless dehydrogenative coupling of N-heterocycles toward functionalized quinolines, phenanthrolines, and indoles.
Regioselective acceptorless dehydrogenative coupling of N-heterocycles toward functionalized quinolines, phenanthrolines, and indoles.
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DOI：
10.1002/anie.201500346
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发表时间：
2015-04
影响因子：
--
通讯作者：
D. Talwar;Angela Gonzalez‐de‐Castro;Ho Yin Li;Jianliang Xiao
中科院分区：
文献类型：
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作者：
D. Talwar;Angela Gonzalez‐de‐Castro;Ho Yin Li;Jianliang Xiao
提出了一种在温和条件下无碱无氧化剂的氮杂环化合物的双偶联反应新策略。在铱催化剂的作用下，N-杂环经历多个sp（3）C H活化步骤，生成亲核烯胺，该亲核烯胺与各种亲电试剂原位反应，得到高度官能化的产物。该偶合反应可与Friedel-Crafts加成反应级联，从而得到N-杂环的双官能化。
A new strategy has been developed for the oxidant- and base-free dehydrogenative coupling of N-heterocycles at mild conditions. Under the action of an iridium catalyst, N-heterocycles undergo multiple sp(3) CH activation steps, generating a nucleophilic enamine that reacts in situ with various electrophiles to give highly functionalized products. The dehydrogenative coupling can be cascaded with Friedel-Crafts addition, resulting in a double functionalization of the N-heterocycles.