Iodine-Promoted Oxidative Cyclization of Methyl Azaarenes and α‑Amino Ketones for One-Pot Synthesis of 2‑Azaaryl-5-aryl Oxazoles

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 hig...

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Bibliographic Details
Published in:Journal of organic chemistry 2022-09, Vol.87 (18), p.12460-12469
Main Authors: Zhu, Yan-Ping, Zhou, Yu, Li, Wen-Juan, Liu, Fu-Rao, Wang, Wen-Cheng, Hao, Kai-Yan, Chao, Bing-Yu, Shi, Tian-Ru, Wu, An-Xin, Sun, Yuan-Yuan
Format: Article
Language:English
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Summary: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.
ISSN:0022-3263
1520-6904
DOI:10.1021/acs.joc.2c01399