Decarboxylative Aminomethylation of Indole-3-carboxylic Acids via Strain Release-Driven Ring Opening of 1,2-Oxazetidines

Org Lett. 2024 Oct 9. doi: 10.1021/acs.orglett.4c03426. Online ahead of print.

Abstract

A copper-catalyzed decarboxylative aminomethylation of indole-3-carboxylic acids with 1,2-oxazetidines has been developed, enabling the rapid synthesis of structurally diverse 3-aminomethylindoles in good to excellent yields. Remarkably, an unprecedented decarboxylative aminomethylation/cyclization cascade was further achieved by a combination of copper and iron salts to construct complex γ-carbolines with high efficiency. It is worth noting that one of the obtained products proved to be a good dual-emissive luminogen, exhibiting both aggregation-caused quenching and aggregation-induced emission.