Having achieved its outstanding professional expertise in medicinal chemistry, compound library design and combinatorial synthesis due to over 20 years’ experience of its leading chemists, Life Chemicals provides high quality library synthesis services in order to support early stages of drug discovery projects of the customers:
Synthesis of Compound Libraries
- based on scaffolds of Life Chemicals
- based on scaffolds of the customer
- design and synthesis of custom targeted libraries
- hit follow-up, hit-to-lead and lead optimization
Up to 1,000 m² of lab space can be allotted for library synthesis and 50 synthetic chemists can be involved (10 PhDs, 28 MSc, 12 BSc). To ensure desired quality of synthesized compounds within the library preparative TLC, NP LC (CombiFlash®) and RP HPLC (Shimadzu®) are used for isolation and purification. The standard purity is 90 % + backed with LCMS and/or NMR analysis data, additional purification can be performed upon customer’s requirements.
Proceeding from our latest investigation results, The Life Chemicals Exclusive Collection of Scaffolds for lead-oriented library synthesis has carefully been designed to include 2,500 unique structures.
These scaffolds are distinguished by the following parameters:
- MW, ClogP, rotatable bonds, Fsp³
- Maximum diversity
- Novelty (better IP position)
- Limited use of amide/sulfonamide couplings
Linked Ring Systems
Fused Ring Systems
Spiro- and Bicyclic Systems
Maintenance of Physicochemical Properties
Average values given below:
MW = 184;
ClogP = – 0.14;
NrotB = 2.17;
Fsp³ = 0.62
provide enough room for lead-oriented library design,
even if rigorous MW/ClogP limitations are applied.