Centre for Catalysis Research and Innovation, Department of Chemistry and Biomolecular Sciences, University of Ottawa, 10 Marie-Curie, Ottawa, Ontario K1N 6N5, Canada.
Org Lett. 2020 Sep 18;22(18):7403-7407. doi: 10.1021/acs.orglett.0c02782. Epub 2020 Sep 3.
Hydroxamic acids are present in a several pharmaceuticals and agrochemicals. Synthetic strategies providing access to hydroxamic acid derivatives remain limited, typically requiring the use of nucleophilic hydroxylamine reagents. Herein, a synthesis of hydroxamates from unactivated carboxylic acids is reported making use of rare blocked (masked) -substituted isocyanates. The applicability of this transformation was highlighted by targeting the synthesis of vorinostat and belinostat derivatives.
羟胺酸存在于几种医药和农用化学品中。获得羟胺酸衍生物的合成策略仍然有限，通常需要使用亲核羟胺试剂。本文报道了一种利用罕见的封闭（掩蔽）取代异氰酸酯从未活化的羧酸合成羟胺酸酯的方法。该转化的适用性通过靶向伏立诺他和贝林司他衍生物的合成得到了强调。
