Peptidic macrocyclization via palladium-catalyzed chemoselective indole C-2 arylation
Peptidic macrocyclization via palladium-catalyzed chemoselective indole C-2 arylation
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DOI：
10.1039/c2cc36962a
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发表时间：
2012-01-01
影响因子：
4.9
通讯作者：
James, Keith
中科院分区：
文献类型：
--
作者：
Dong, Huijun;Limberakis, Chris;James, Keith
通过钯催化色氨酸侧链与含卤代苯基氨基酸的C-H芳基化反应，发展了一种高效的大环化反应。该方法允许以40-75%的产率在中等浓度下直接获得15-至25-元联芳基大环，其中C-H芳基化仅在色氨酸吲哚的C-2位进行。
A highly efficient macrocyclization reaction has been developed via the palladium-catalyzed C-H arylation of the side-chains of tryptophan with halophenyl-containing amino acids. This method allows for direct access to 15- to 25-membered biaryl macrocycles in 40-75% yield, at moderate concentration, with C-H arylation proceeding exclusively at the C-2 position of the tryptophan indole.