Modular Total Synthesis of Protein Kinase C Activator (−)-Indolactam V

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• 作者：Jeremy Haynes-Smith ; Italia Diaz ; Kelvin L. Billingsley
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：May 6, 2016
• 年：2016
• 卷：18
• 期：9
• 页码：2008-2011
• 全文大小：336K
• 年卷期：0
• ISSN：1523-7052

文摘

A concise, eight-step total synthesis of (−)-indolactam V, a nanomolar agonist of protein kinase C, is reported. The synthesis relies upon an efficient copper-catalyzed amino acid arylation to establish the indole C4–nitrogen bond. This cross-coupling method is applicable to a range of hydrophobic amino acids, providing a platform for further diversification of indolactam alkaloid scaffolds and studies on their potent biological activity.