The Suzuki-Miyaura cross-coupling reaction has revolutionized the way chemists make carbon-carbon bonds. However, the method is primarily employed to construct Csp2–Csp2 bonds resulting in flat molecules, which have lower bioactivity and selectivity compared to their three-dimensional counterparts. As these molecules populate pharmaceutical libraries, they inhibit the discovery of valuable new drug candidates. In this talk, our work enabling the introduction of chirality into the Suzuki-Miyaura cross-coupling reaction will be presented, including work using compounds with predetermined chirality, both in the nucleophile or electrophile. Work on the development of novel electrophiles based on sulfones will illustrate the versatility of these novel molecules in cross-coupling chemistry.
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