Bauer Adriano, Maulide Nuno
Institute of Organic Chemistry , University of Vienna , Währinger Straße 38 , 1090 Vienna , Austria . Email:
Chem Sci. 2019 Sep 10;10(42):9836-9840. doi: 10.1039/c9sc03715b. eCollection 2019 Nov 14.
Aliphatic C-H functionalization is a topic of current intense interest in organic synthesis. Herein, we report that a facile and stereoselective dehydrogenation event enables the functionalization of aliphatic amides at different positions in a one-pot fashion. Derivatives of relevant pharmaceuticals were formally functionalized in the β-position in late-stage manner. A single-step synthesis of incrustoporine from a simple precursor further showcases the potential utility of this approach.
脂肪族C-H官能化是当前有机合成中备受关注的一个话题。在此，我们报道了一种简便且立体选择性的脱氢反应，能够以一锅法实现脂肪族酰胺不同位置的官能化。相关药物的衍生物在后期以β-位进行了形式上的官能化。从一个简单前体一步合成硬壳孢菌素进一步展示了这种方法的潜在效用。
