Synthesis of indolines via a domino Cu-catalyzed amidation/cyclization reaction
Synthesis of indolines via a domino Cu-catalyzed amidation/cyclization reaction
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DOI：
10.1021/ol8008792
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发表时间：
2008-07-03
期刊：
影响因子：
5.2
通讯作者：
Buchwald, Stephen L.
中科院分区：
文献类型：
--
作者：
Minatti, Ana;Buchwald, Stephen L.
基于多米诺铜催化的酰胺化/亲核取代反应，发展了一种高效的一锅法合成吲哚啉及其同系物的方法。取代的2-碘苯乙基甲磺酸酯和相关化合物以优异的产率得到相应的产物。当在反应条件下转化对映体纯的甲磺酸酯时，没有观察到光学纯度的侵蚀。
A highly efficient one-pot procedure for the synthesis of indolines and their homologues based on a domino Cu-catalyzed amidation/nucleophilic substitution reaction has been developed. Substituted 2-iodophenethyl mesylates and related compounds afforded the corresponding products in excellent yields. No erosion of optical purity was observed when transforming enantiomerically pure mesylates under the reaction conditions.