Discovery Chemistry Group, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Org Lett. 2017 Jul 7;19(13):3616-3619. doi: 10.1021/acs.orglett.7b01606. Epub 2017 Jun 27.
The preparation of substituted azaindolines utilizing a domino palladium-catalyzed Heck cyclization/Suzuki coupling is described. The approach is amenable for the construction of all four azaindoline isomers. A range of functional groups such as esters, amides, ketones, sulfones, amines, and nitriles are all tolerated under the reaction conditions.
本文描述了一种利用多步钯催化 Heck 环化/Suzuki 偶联反应制备取代氮茚的方法。该方法适用于所有四种氮茚异构体的构建。在反应条件下，各种官能团，如酯、酰胺、酮、砜、胺和腈，都能被容忍。
