Research demonstrates effective copper-based catalyst for cross-coupling in drug synthesis, indicating improved safety and efficiency.
The synthesis, in particular the industrial production, of pharmaceuticals requires a broad arsenal of synthetic reactions capable of selectively forming specific structural motifs and assembling smaller building blocks into complex molecules. The Chan–Evans–Lam cross-coupling reaction, which forms a bond between a N-nucleophile and an aryl group from a boronic acid, catalysed by copper salts, is a typical example of this synthetic route. Considering the toxicity of copper and the stringent regulatory limits for its residues in final pharmaceutical products, a heterogeneous catalytic approach offers a viable alternative for this transformation. In this work, we present a simply and reproducibly synthesized catalyst based on copper nanoparticles supported on reduced graphene oxide (Cu-rGO), with high efficiency in a model Chan–Lam reaction involving benzimidazole and aniline derivatives with substituted boronic acids.
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Stehlík et al. (2026) studied this question.
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