The scientific development in the area of enantioseparation during the last few decades has centered on the production of new chiral stationary phases (CSPs) and new chiral derivatizing reagents (CDRs) for use in liquid chromatography, and in particular high-performance liquid chromatography (HPLC) only. Both CSPs and CDRs have several limitations which, in general, are ignored. Little attention has been paid to thin-layer chromatography (TLC) despite its many advantages compared to HPLC in pharmaceutical and drug analysis and the areas of natural products chemistry and organic synthesis, particularly enantioselective synthesis in purification of the product prior to establishing enantiomeric ratio by different method(s). TLC provides a rapid, easy, aff ordable, and simple approach in all these situations. The demonstrated capability and effi- ciency of TLC in direct resolution of the racemate clearly establish its superiority, and the methodology should allow its application in the resolution of several other racemates, irrespective of the functional group, in a very short time along with the recovery of native enantiomers (for further use).