Leveraging conformational control to access sp2-rich 3D platforms for drug discovery

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Introducing a bulky ortho-substituent to sp2- rich amides or biaryls gives rise to two enantiomers, which can show drastically different pharmacokinetic and pharmacodynamic properties. Typically, a large tert-butyl group is required to prevent racemisation of these 3D compounds, however the high lipophilicity of this group limits its applications in drug discovery. This project focuses on replacing this group with more medicinally relevant locking groups.