Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education, Department of Chemistry & Materials Science, Northwest University, Xi'an 710069, China.
Org Lett. 2021 Mar 5;23(5):1921-1927. doi: 10.1021/acs.orglett.1c00365. Epub 2021 Feb 19.
A direct and efficient palladium-catalyzed oxidative dehydrogenative fluoroalkoxylation of benzaldehydes is reported here for the first time. The method features mild reaction conditions, good tolerance of functional groups, and a broad substrate scope. The protocol employs the transient directing group strategy, thereby avoiding the additional installation and removal of directing groups, endowing the method with great advantages of atom and step economy. The approach should find broad applications in drug synthesis and discovery processes.
本文首次报道了一种直接高效的钯催化氧化脱氢氟烷氧基化苯甲醛的方法。该方法具有反应条件温和、官能团容忍性好、底物范围广等特点。该方案采用瞬态导向基团策略，从而避免了导向基团的额外安装和去除，使该方法具有原子经济性和步骤经济性的巨大优势。该方法应该在药物合成和发现过程中有广泛的应用。
