Rhodaelectro-catalyzed access to chromones via formyl C–H activation towards peptide electro-labeling

作者：Maximilian Stangier, Antonis M. Messinis, João C. A. Oliveira, Hao Yu, Lutz Ackermann · 发表于：Nature Communications · 年份：2021 · DOI：10.1038/s41467-021-25005-8 · 被引用次数：62 · 研究领域：Catalytic C–H Functionalization Methods、Radical Photochemical Reactions、Sulfur-Based Synthesis Techniques

Chromones represent a privileged scaffold in medicinal chemistry and are an omnipresent structural motif in natural products. Chemically encoded non-natural peptidomimetics feature improved stability towards enzymatic degradation, cell permeability and binding affinity, translating into a considerable impact on pharmaceutical industry. Herein, a strategy for the sustainable assembly of chromones via electro-formyl C-H activation is presented. The rational design of the rhodaelectro-catalysis is guided by detailed mechanistic insights and provides versatile access to tyrosine-based fluorogenic peptidomimetics.