Defining and testing enantiomerically pure building blocks and final products for the production of API’s is a crucial part of drug development, given the considerable differences observed in vivo for many biologically active enantiomers. Of the many rapid chiral screening options available, classical resolution of diastereoisomeric salts, via fractional crystallisation, remains one of the most cost effective and robust methods.
As a company we have a proven track record of taking chiral screening projects from their initial research phases and successfully delivering methodology for kilo scale production of enantiopure material within a GMP environment. Our approach is to investigate in parallel a wide range of experimental space, utilising our customised crystallisation platform. By simultaneously covering a range of commercially viable resolving agents, used in varying stoichiometries and in a range of solvent and co-solvent mixtures we rapidly assess whether such chiral resolution is possible. Having defined a suitable salt candidate (or candidates) and a process, systematic scale-up of the method would be performed in order to ensure a satisfactory transition to large scale production.
