Myriad Aryne Derivatives from Carboxylic Acids
Summary
Researchers report a practical aryne precursor made in a single step from common carboxylic acids. The precursor is activated by blue light or heat to deliver a wide range of aryne derivatives — including numerous previously unknown aminated arynes and pyridynes — broadening the synthetic reach of aryne chemistry and lowering the barrier to use in drug discovery. Supplementary information includes complete experimental procedures, characterisation and DFT mechanistic studies.
Key Points
- Aone-step derivatisation converts widely available carboxylic acids into stable aryne precursors.
- Activation by blue light or thermal methods produces diverse aryne species, including aminated arynes and pyridynes.
- The approach overcomes longstanding practical hurdles in generating arynes, making them more accessible beyond specialist labs.
- Methodology is directly relevant to medicinal-chemistry and agrochemical programmes seeking densely substituted aromatic scaffolds.
- Extensive supplementary materials provide experimental details, compound characterisation and mechanistic (DFT) evidence.
Why should I read this
Quick and to the point — if you make aromatic molecules, this paper gives you a much easier way to access arynes from everyday carboxylic acids. It turns a niche, fiddly technique into something your med-chem team can actually use. Read it for a practical trick that could speed up synthesis and unlock new substitution patterns.