Silicon-Containing Building Blocks for Drug Design
Silicon-containing compounds have been largely ignored in drug design until recently. Silicon can be considered a bioisostere of carbon and hence offers an innovative avenue in drug discovery. For example, C/Si exchange in drug-like scaffolds provides an exciting approach in medicinal chemistry to improve ADME/Tox profile and to enhance potency of the biologically active compounds. Herein we have designed and synthesized a library of silicon-containing building blocks for drug design.
Case studies
Advantages of “Silicon Switch”:
- Bond length C–C = 1.54 Å, C–Si = 1.87 Å → changes in the interactions with specific proteins;
- Increase in lipophilicity;
- Si prefers higher coordination numbers → access to compounds for which corresponding carbon analogs are not available.
We offer
More than 30 of silicon-containing building blocks from stock on a 5-10 g scale.
MedChem Highlights
- Aliphatic Pinacol Boronates for Medicinal Chemistry
- Deuterium-Containing Building Blocks for Drug Design
- Analogues of Piperidine for Drug Design
- 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