Chiral resolution

Diastereomeric salts and chiral co-crystals formation

Most drug candidates have chiral centres in their structure. Generally only one of the enatiomers has got the sought-after biological activity, thus a separation of both enantiomers is necessary to have a higher activity in lower doses and to avoid regulatory issues, as the presence of the other enantiomer may sometimes lead to undesired secondary effects.

Crysforma has successfully applied its in-house developed salt screening methodology to the resolution of chiral molecules with ionization sites through diastereomeric salt formation. In a similar way, non-ionisable chiral molecules can also be resolved by formation of co-crystals with chiral coformers.

Type of studies:

  • Crystallization screening to discover the optimal chiral resolution agent and crystallization solvent
  • Scale-up of the resolution process.
  • Development of HPLC analytical methods to determine the enantiomerical excess
  • Determination of absolute configuration by single crystal X-ray diffraction of enantiomerically pure compounds