碘促进的甲基氮杂芳烃和α-氨基酮的氧化环化反应一锅法合成 2-氮杂芳基-5-芳基恶唑
Iodine-Promoted Oxidative Cyclization of Methyl Azaarenes and α-Amino Ketones for One-Pot Synthesis of 2-Azaaryl-5-aryl Oxazoles.
机构信息
School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Shandong Yantai, 264005, P. R. China.
Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Hubei Wuhan, 430079, P. R. China.
出版信息
J Org Chem. 2022 Sep 16;87(18):12460-12469. doi: 10.1021/acs.joc.2c01399. Epub 2022 Sep 6.
A high efficiency protocol was developed for the synthesis of 2,5-disubstituted oxazoles via iodine-promoted oxidative domino cyclization. These reactions were performed with readily available methyl azaarenes and α-amino ketones under metal-free conditions. This protocol is a simple method with high functional group compatibility, a wide range of substrates, and excellent yield, providing a new way to synthesize azaarene-attached oxazoles.
开发了一种高效的合成 2,5-二取代恶唑的方法，通过碘促进的氧化级联环化反应实现。这些反应在无金属条件下，使用易得的甲基氮杂芳烃和α-氨基酮进行。该方法具有反应条件温和、官能团兼容性好、底物范围广、产率高等优点，为氮杂芳烃连接的恶唑类化合物的合成提供了一种新方法。
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