Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Bristol Myers Squibb, Small Molecule Drug Discovery, 200 Cambridge Park Drive, Cambridge, MA 02140, USA.
Angew Chem Int Ed Engl. 2023 Jan 23;62(4):e202214153. doi: 10.1002/anie.202214153. Epub 2022 Dec 15.
The site-selective palladium-catalyzed three-component coupling of unactivated alkenyl carbonyl compounds, aryl- or alkenylboronic acids, and N-fluorobenzenesulfonimide is described herein. Tuning of the steric environment on the bidentate directing auxiliary enhances regioselectivity and facilitates challenging C(sp )-F reductive elimination from a Pd intermediate to afford 1,2-carbofluorination products in moderate to good yields.
本文描述了未活化的烯基羰基化合物、芳基或烯基硼酸和 N-氟代苯磺酰胺之间的钯催化的位点选择性三组分偶联反应。双齿导向辅助基的空间环境的调节可以增强区域选择性，并有利于从 Pd 中间体中进行具有挑战性的 C(sp3)-F 还原消除，从而以中等至良好的收率得到 1,2-碳氟化合物产物。
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