Enantiomeric Separation of Privileged Scaffold Derivatives in Early Drug Discovery Using Chiral SFC Application Note

In the work discussed here, we assess the success rate of doing chiral separations at the earliest “hit-to-lead” stage of drug discovery research. “Hit compounds” identified in HTS screens are often from libraries of small molecules available commercially from specialized companies that support small molecule drug discovery research. To mimic this process we used the same source of compounds for our study. The compounds were screened by SFC for the purpose of developing preparative purification methods and also by HPLC in cases where SFC did not provide adequate separation and for the purpose of analyzing purity post-purification.