A team of scientists led by Dr. Manuel van Gemmeren, Otto Hahn research group leader of the MPI CEC at the Westfälische Wilhelms-Universität Münster, has developed a synthetic method, which enables the direct introduction of alkyne groups, which are relevant for example in the context of medicinal chemistry, into aromatic substrates.
Remarkably, the regioselectivity of this C–H alkynylation is predominantly controlled by steric rather than electronic properties of the substrate. This gives access to derivatives - even of complex substrates - which could not be accessed or would be much more challenging to access using conventional methods.
The research results were recently published in the Journal of the American Chemical Society (JACS).
Mondal, A., Chen, H., Flaemig, L., Wedi, P., van Gemmeren, M. (2019). Sterically Controlled Late-Stage C-H Alkynylation of Arenes Journal of the American Chemical Society https://doi.org/10.1021/jacs.9b10868