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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 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.

Discovery of Brigatinib

P(O)Me2-group:

  • chemically stable;
  • metabolically stable;
  • H-bond acceptor;
  • increases solubility;
  • decreases lipophilicity.

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>30 unique P(O)Me2-containing derivatives on a 5-50 g scale from our stock.

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