P(O)Me2-containing Building Blocks for Drug Design

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

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Discovery of Brigatinib

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