Normandie Université, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000, Rouen, France.
Industrial Research Centre-Oril Industrie, CS 60125, 76210, Bolbec, France.
Chemistry. 2021 Oct 7;27(56):13961-13965. doi: 10.1002/chem.202102411. Epub 2021 Sep 12.
An efficient primary-amine-directed, palladium-catalyzed C-H halogenation (X=I, Br, Cl) of phenylalanine derivatives is reported on a range of quaternary amino acid (AA) derivatives thanks to suitable conditions employing trifluoroacetic acid as additive. The extension of this original native functionality-directed ortho-selective halogenation was even demonstrated with the more challenging native phenylalanine as tertiary AA.
本文报道了在三氟乙酸添加剂存在下，通过适宜的条件，实现了一系列季铵盐氨基酸衍生物的高效、钯催化、芳基氨基酸导向的 C-H 卤化反应（X=I、Br、Cl）。该方法甚至可以将更具挑战性的天然氨基酸苯丙氨酸作为三级氨基酸进行扩展，实现了原始的固有功能导向的邻位选择性卤化。
