Phosphine Oxides (-POMe) for Medicinal Chemistry: Synthesis, Properties, and Applications.

A general practical approach to hetero(aromatic) and aliphatic P(O)Me-substituted derivatives is elaborated. The key synthetic step was a [Pd]-mediated C-P coupling of (hetero)aryl bromides/iodides with HP(O)Me. The P(O)Me substituent was shown to dramatically increase solubility and decrease lipophilicity of organic compounds.