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Enantiomer Resolution Screening

The different bioactivities of enantiomers (optical isomers) are of the utmost importance in the manufacture of active pharmaceutical ingredients (APIs). There are numerous examples where two enantiomers can show marked differences in their pharmacological effects. Enantiomerically purified compounds are therefore often key building blocks in the synthesis of APIs. The main challenge is to find a suitable separation method within a short time.

The most practical and the most frequently applied method for preparing pure enantiomers is the optical resolution of racemates (also often referred to as 'classical resolution') through the formation and separation of diastereomeric salts. In this strategy, an acid-base reaction is involved between a racemate and a resolving agent, which is in practice an enantiopure (single) enantiomer. When the solubilities of the two diastereomeric salts that are formed are very different, one of the salts is insoluble and can be filtered out of the mixture, leaving the other in the solution (in the most ideal case). Finally, the salt is decomposed by treatment with either acid or base, and the resolving agent can be recovered.

Avantium has developed an automated, efficient and fast screening method to identify suitable resolving agents / solvent combinations for a given substrate (either acidic or basic).