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.
Discovery of Brigatinib
>100 unique P(O)Me2-containing derivatives on a 5-50 g scale from our stock.