Eduardo de Pedro Beato; Julián Priego; Adrián Gironda-Martínez; Fernando González; Jesús Benavides; Jesús Blas; María Dolores Martín-Ortega; Miguel Ángel Toledo; Jesús Ezquerra; Alicia Torrado
ACS Comb. Sci., 2019, 21, 2, 69-74
https://doi.org/10.1021/acscombsci.8b00142

Abstract

DNA-encoded library technology (ELT) has emerged in the pharmaceutical industry as a powerful tool for hit and lead generation. Over the last 10 years, a number of DNA-compatible chemical reactions have been published and used to synthesize libraries. Among the most commonly used reactions in medicinal chemistry is the C–N bond formation, and its application to DNA-encoded library technology affords an alternative approach to identify high-affinity binders for biologically relevant protein targets. Herein we report a newly developed Pd-promoted C–N cross coupling reaction between DNA-conjugated aryl bromides and a wide scope of arylamines in good to excellent yields. The mild reaction conditions should facilitate the synthesis of novel DNA-encoded combinatorial libraries.