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在自由基条件下由联芳基-2-草氨酸合成菲啶酮的无过渡金属方法

Transition-metal-free synthesis of phenanthridinones from biaryl-2-oxamic acid under radical conditions.

作者信息

Yuan Ming, Chen Li, Wang Junwei, Chen Shenjie, Wang Kongchao, Xue Yongbo, Yao Guangmin, Luo Zengwei, Zhang Yonghui

机构信息

Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology , Wuhan 430030, People's Republic of China.

出版信息

Org Lett. 2015 Jan 16;17(2):346-9. doi: 10.1021/ol503459s. Epub 2015 Jan 8.

DOI:10.1021/ol503459s
PMID:25569786
Abstract

Na2S2O8-promoted decarboxylative cyclization of biaryl-2-oxamic acid for phenanthridinones has been developed. This work illustrates the first example of intramolecular decarboxylative amidation of unactivated arene under transition-metal-free conditions. Additionally, this approach provides an efficient and economical method to access biologically interesting phenanthridinones, an important structure motif in many natural products.

摘要

已开发出Na2S2O8促进的联芳基-2-草酰胺酸脱羧环化反应以制备菲啶酮。这项工作展示了在无过渡金属条件下未活化芳烃分子内脱羧酰胺化的首个实例。此外,该方法为获得具有生物学意义的菲啶酮提供了一种高效且经济的方法,菲啶酮是许多天然产物中的重要结构基序。

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