Md Imdadul H. Khan, Jiaxin Yang, Seong Jong Kim, Hoang V. Le
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引用次数: 0
摘要
报告采用 Togni 试剂 II 和 umpolung 策略对酰胺进行了 α-C-H 加氧反应。在温和、无催化剂的反应条件下,以叔胺为原料制备了中高产率的α-苯甲酰氧基酰胺。所有试剂均可从市场上买到,易于使用,并与各种官能团和环兼容。α-苯甲酰氧基酰胺可以很容易地转化为相应的α-羟基酰胺,几乎达到定量收率。这种转化在合成医药和农业领域的重要化合物方面具有巨大潜力。
A mild and catalyst-free α-benzoyloxylation of tertiary amides
An α-C–H oxygenation of amides using Togni reagent II and an umpolung strategy is reported. α-Benzoyloxy amides were prepared in moderate-to-high yields from tertiary amides under mild and catalyst-free reaction conditions. All reagents are commercially available, easy to use, and compatible with various functional groups and rings. α-Benzoyloxy amides could be easily transformed into the corresponding α-hydroxy amides in almost quantitative yields. This transformation has significant potential for the synthesis of important compounds in pharmaceutical and agricultural fields.
期刊介绍:
Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.