Department of Nanopharmaceutical Sciences and Department of Life Science and Applied Chemistry, Nagoya Institute of Technology, Gokiso, Showa-ku, Nagoya 466-8555, Japan.
Institute of Advanced Fluorine-Containing Materials, Zhejiang Normal University, 688 Yingbin Avenue, Jinhua 321004, China.
Org Lett. 2021 Feb 5;23(3):847-852. doi: 10.1021/acs.orglett.0c04087. Epub 2021 Jan 19.
We describe a novel reagent system to obtain acyl fluorides directly from three different functional group precursors: carboxylic acids, aldehydes, or alcohols. The transformation is achieved via a combination of trichloroisocyanuric acid and cesium fluoride, which facilitates the synthesis of various acyl fluorides in high yield (up to 99%). It can be applied to the late-stage functionalization of natural products and drug molecules that contain a carboxylic acid, an aldehyde, or an alcohol group.
我们描述了一种从三种不同官能团前体(羧酸、醛或醇)直接获得酰氟的新型试剂系统。该转化通过三氯异氰尿酸和氟化铯的组合来实现,可高收率(高达 99%)合成各种酰氟。它可以应用于含有羧酸、醛或醇基团的天然产物和药物分子的后期功能化。