Phosphine oxides belong to a chemical class seldom employed in drug design. However, the FDA-approval of <i>Brigatinib</i> drug (ARIAD Pharm.) in 2017 may further inspire application of this unique functional group in medicinal chemistry. The highly ionic P=O bond imparts a number of important drug-like properties, including decreased lipophilicity, increased aqueous solubility, H-bond acceptor ability, and high metabolic stability. Herein we have designed and synthesized a library of phosphine oxide derivatives for drug design.

P(O)Me<sub>2</sub>-containing building blocks for drug design

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

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P(O)Me2-containing building blocks for drug design

P(O)Me₂-containing building blocks for drug design