Boron-containing heterocyclic scaffolds with active halogens

The Suzuki–Miyaura cross-coupling of boronic acid derivatives is one of the most used reactions in organic and medicinal chemist's toolbox. The rapid advancement of this method resulted in its efficient application for the late-stage modification of biologically active substrates and construction of combinatorial libraries. Herein, we offer a library of heterocyclic boronic esters with active halogen atoms. They can be used for metal-mediated cross-coupling reactions followed by the stepwise a nucleophilic aromatic substitution (S_NAr) to produce functionalized products.