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Late-stage diversifi cation by rutheniumelectro-catalyzed C¨CH mono- and di-acyloxylation
Green Synthesis and Catalysis ( IF 8.2 ) Pub Date : 2020-12-1 , DOI: 10.1016/j.gresc.2020.10.002
Haiwei Shen , Didi Cheng , Yujin Li , Tao Liu , Xiao Yi , Lei Liu , Fei Ling and Weihui Zhong

A ruthenium-catalyzed electrochemical dehydrogenative C(sp2) H acyloxylation of aniline derivatives with carboxylic acids has been developed. Electric current is used to recycle the active ruthenium-based catalyst and promote H2 evolution. This method significantly expands the scope and enhances the selectivity of metal-electron catalyzed mono- and di-acyloxylations, which remain challenged. Our findings allowed mono-selectivity in broadly effective late-stage diversification of structurally complex drugs and natural product molecules, tolerating drugs, natural products and amino acids. The method and its underlying strategy are expected to have widespread uses in functional aniline synthesis and drug discovery process.

中文翻译:

钌电催化的CCH单-和二-酰氧基化的后期分散

已经开发了钌催化苯胺衍生物与羧酸的电化学脱氢C(sp2)H酰氧基化反应。电流用于回收活性钌基催化剂并促进H2的释放。该方法显着扩大了范围,并增强了仍然受到挑战的金属电子催化的单酰基和二酰基氧基化的选择性。我们的发现允许在结构复杂的药物和天然产物分子,耐受药物,天然产物和氨基酸的广泛有效的后期多样化中进行单选择性。该方法及其潜在策略有望在功能性苯胺合成和药物发现过程中得到广泛应用。
更新日期:2020-12-28
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