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.
We offer
>30 unique P(O)Me2-containing derivatives on a 5-50 g scale from our stock.
MedChem Highlights
- Building blocks and linkers for PROTAC synthesis
- Heterocyclic Sulfonyl Fluorides
- Silicon-Containing Building Blocks
- Epoxides for Drug Design
- Analogues of CF3-Pyridine for Drug Design
- Piperazine Bioisosteres for Drug Design
- Sugar-like Building Blocks for Drug Design
- Cyclic Sulfonamides for Drug Design
- Morpholine Bioisosteres for Drug Design
- P(O)Me2-containing Building Blocks for Drug Design
- Saturated Bioisosteres of ortho-/meta-substituted Benzenes
- Saturated bioisosteres of para-substituted benzenes
- Sulfonyl fluorides (-SO2F)
- Diazirines
- Oxetane-containing Building Blocks
- SF5-Building Blocks
- Stannanes for coupling reactions
- Sulfoximines for Drug Design
- Saturated Bioisosteres of Benzene
- Heterocyclic scaffolds
- Macrocycles
- Azide-linkers for Drug Design
- Unnatural Amino Acids
- Cubane-containing building blocks
- Benzoxaboroles for Drug Design