Department of Chemistry, Scripps Research, 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Org Lett. 2020 Oct 2;22(19):7594-7598. doi: 10.1021/acs.orglett.0c02799. Epub 2020 Sep 17.
An operationally simple method to employ nonactivated carboxylic acids as alkylating agents in the -alkylation of heterocycles is reported through an electrochemically driven anodic decarboxylative process. A wide substrate scope across a range of heterocycles is demonstrated along with a series of applications that significantly reduce the step count required to access such medicinally relevant structures.
通过电化学驱动的阳极脱羧反应,报道了一种操作简单的方法,可将未活化的羧酸作为烷基化试剂用于杂环的-烷基化反应。该方法展示了广泛的杂环底物范围,并进行了一系列应用,显著减少了获得此类具有药物相关性结构所需的步骤数。