电化学形成 N-酰氧基酰胺基自由基及其应用：sp 和 sp~C-H 键的区域选择性分子内胺化。
Electrochemical Formation of N-Acyloxy Amidyl Radicals and Their Application: Regioselective Intramolecular Amination of sp and sp C-H Bonds.
机构信息
College of Chemistry and Pharmaceutical Engineering , Nanyang Normal University , Nanyang , 473061 , China.
College of Life Science & Bioengineering , Beijing University of Technology , Beijing 100124 , China.
出版信息
Org Lett. 2018 Jun 15;20(12):3443-3446. doi: 10.1021/acs.orglett.8b00981. Epub 2018 Jun 4.
Electrochemical generation of N-acyloxy amidyl radicals via an inner-sphere electron-transfer process is described for the first time. With NaBr as the catalyst and electrolyte, the in situ generated amidyl radicals undergo intramolecular C(sp/sp)-H aminations to give lactams with unprecedented regio- and chemoselectivities. Moreover, the synthetic utility of current method is demonstrated by the synthesis of PJ34 and Phenaglaydon.
首次描述了通过内球电子转移过程电化学产生 N-酰氧基氨酰基自由基。以 NaBr 作为催化剂和电解质，原位生成的氨酰基自由基进行分子内 C(sp/sp)-H 胺化反应，以空前的区域和化学选择性得到内酰胺。此外，通过 PJ34 和 Phenaglaydon 的合成本法的合成实用性得到了证明。
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