Marco Potowski; Ricarda Lüttig; Alexandros Vakalopoulos; Andreas Brunschweiger
Org. Lett., 2021, 23(14), 5480-5484
https://doi.org/10.1021/acs.orglett.1c01834

Abstract

DNA-encoded libraries designed around heterocyclic scaffolds have proven highly productive in target-based screening. Here, we show the synthesis of imidazopyridines on a controlled pore glass-coupled DNA oligonucleotide for solid phase-initiated encoded library synthesis. The target compounds were synthesized by a variant of the A3 coupling reaction from aminopyridines, alkynes, and aldehydes promoted by copper(I/II) and furnished diverse substituted scaffolds with functionalities for library design. Although proceeding under forcing conditions, it produced minimal DNA damage.