Stereoselective Peptide Modifications via β-C(sp3)-H Arylations

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• 作者：Biplab Mondal ; Brindaban Roy ; Uli Kazmaier
• 刊名：Journal of Organic Chemistry
• 出版年：2016
• 出版时间：December 2, 2016
• 年：2016
• 卷：81
• 期：23
• 页码：11646-11655
• 全文大小：533K
• ISSN：1520-6904

文摘

Palladium-catalyzed stereoselective β-arylations of phenylalanine, proline- and pipecolinic acid-containing peptides are a versatile tool for peptide modifications. The reactions proceed without epimerization of stereogenic centers in the peptide chain. If suitable functionalized aryl iodides are introduced, subsequent cross coupling reactions can be used for further modifications. The 8-amino quinoline (AQ) directing group can easily be removed, allowing the prolongation of the peptide chain at the C-terminus.