Institute of Organic Chemistry, Faculty of Chemistry, University of Vienna , Währinger Straße 38, 1090 Vienna, Austria.
J Am Chem Soc. 2017 May 17;139(19):6578-6581. doi: 10.1021/jacs.7b02983. Epub 2017 May 9.
A suite of flexible and chemoselective methods for the transition-metal-free oxidation of amides to α-keto amides and α-hydroxy amides is presented. These highly valuable motifs are accessed in good to excellent yields and stereoselectivities with high functional group tolerance. The utility of the method is showcased by the formal synthesis of a potent histone deacetylase inhibitor.
本文提出了一系列灵活且具有化学选择性的方法，可实现酰胺到 α-酮酰胺和 α-羟基酰胺的无过渡金属氧化。这些具有高价值的结构单元具有良好到优异的产率和立体选择性，并且对官能团具有高耐受性。该方法的实用性通过一种有效的组蛋白去乙酰化酶抑制剂的形式合成得到了展示。
