Direct Alkenylation of Vinyl Halides: Reaction Discovery through High-Throughput Experimentation




Cruise, Odhran

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A broadly applicable method for carbon-carbon bond formation via carbon-hydrogen bond activation has been developed using palladium catalysis. This transformation couples aromatic heterocycles and vinyl halides in a direct alkenylation reaction. High-throughput experimentation techniques were used to conduct multivariate testing methods to rapidly assess and optimize chemical systems across a broad range of substrates. Compared to traditional methods, high-throughput experimentation allows researchers to run arrays of reactions in parallel reducing timelines from months to days. High-throughput methods were throughout the entire process, from reaction discovery to preparative scale optimization, enabling faster drug discovery timelines in the pharmaceutical industry. The products resulting from the transformation developed are biologically active and contain synthetic handles for further functionalization. This enables researchers to expand the potential scope of products for applications in the pharmaceutical industry.



high-throughput experimentation, industrial collaboration, chemistry, Science