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
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>100 unique P(O)Me2-containing derivatives on a 5-50 g scale from our stock.
MedChem Highlights
- SnAP Reagents
- Fluoroalkyl ethers for Drug Design
- N-Nitrosamines
- N-Trifluoromethyl Azoles for Drug Discovery
- Cyclic sulfates and sulfamidates as alkylating reagents
- Saturated Bioisosteres for ortho-substituted Benzenes
- Aliphatic Trifluoroborates (-BF3) for C-C couplings
- Functionalized Vinyl Boronates for C-C couplings
- Unique 3D-shaped Spirocycles
- Water-soluble non-classical benzene mimics
- gem-Difluorinated Amines for Drug Design
- Fluorosulfates and Sulfamoyl Fluorides
- Alkyne-containing Linkers
- Structurally optimized tetrazines for rapid biological labeling
- 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
- 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
- Heterocyclic scaffolds
- Azide-linkers for Drug Design
- Unnatural Amino Acids
- Cubanes for Medicinal Chemistry
- Benzoxaboroles for Drug Design