ArticleAngewandte Chemie (International ed. in English)2026
Remapping the Synthetic Landscape of α-Tertiary Alkylamines via Dual-Functional Catechol.
Article in Angewandte Chemie (International ed. in English), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
α-Tertiary alkylamines are privileged motifs with a strong propensity to be bioactive, rendering their efficient synthesis fundamentally important across diverse areas of chemistry. Despite recent advances in aliphatic amine preparation, the direct construction of hindered α-tertiary amines remains a long-standing challenge. Here, we report a three-component assembly that exploits the dual role of catechol to enable the modular synthesis of these motifs from readily available, bench-stable reactants. This method exhibits exceptional functional-group tolerance and provides access to a variety of synthetically demanding molecular architectures, including consecutive quaternary centers as well as vicinal aminoether and diamine fragments. This approach, therefore, represents a valuable supplement to the chemist's toolbox for α-tertiary alkylamines, offering streamlined routes to complex targets and significant possibilities in drug discovery.
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