From racemic epichlorohydrin to a single enantiomer of the drug timolol maleate

Stereoselective Crystallization as a Basis for Single‐Enantiomer Drug Production

“…Diol 15 crystallizes as an ideal normal conglomerate and oxirane is a conglomerate with a partial solid solution . Both compounds were used by us in the original synthesis of the single enantiomer timolol from common raw material, racemic epichlorohydrin .…”

“…We believe that in this regard our proposed approach may be helpful. The key step of this is the deracemization of the conglomerate formative rac-(2,6-dimethylphenoxy)propane-1,2-diol 24 using the entrainment procedure [83].…”

Solubility- and melting-based approaches to evaluate the inner-crystal enantiophobia and enantiophilia undergoing a structural change within a homologous series, exemplified by chiral glycerol ethers

“…7,8 Furthermore, comprehending the phase behaviour of a chiral system allows for the purification of a substance, whether it is a target product or a precursor, and the enrichment of a solid sample or mother liquor with a desired enantiomer in a physically justified manner. [9][10][11] Identifying the relationship between structure and property is crucial in understanding homochiral crystallisation. This understanding can lead to the design of molecules with enantiophobic properties.…”

“…7,8 Furthermore, comprehending the phase behaviour of a chiral system allows for the purification of a substance, whether it is a target product or a precursor, and the enrichment of a solid sample or mother liquor with a desired enantiomer in a physically justified manner. 9–11…”