N-linked azoles have a rich history as isosteric replacements for a variety of aromatics in both crop protection and medicinal chemistry. They can stand in for either meta- or para-substituted benzenes and heterocycles depending upon the situation. When substituted on methylenes, they can be effective replacements for benzylic and phenoxy residues. More recently trifluoromethylazoles have been used as lipophilic electron withdrawing aromatic substituents. Additionally N-linked azoles possess interesting chemical properties, they can be both leaving groups and activate proximal leaving groups for displacement. Selected examples from the past 30 years of research across the industry will be highlighted.

N-linked azoles as design elements in bioactive molecules

256th National Meeting (2018)

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