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Optically active 2‐aryl‐1,3‐oxazolines, such as aromaticcarbocycles, heterocycle‐binding 4‐benzyl (or phenyl)‐1,3‐oxazolines and their 5‐benzyl (or phenyl)‐1,3‐oxazoline isomers were successfully prepared through a bromotriphenylphosphonium salt promoted aziridine ring formation and ring opening sequential process involving tandem one‐pot cyclization of chiral 2‐amino‐3‐phenylpropanol or 2‐amino‐2‐phenylethanol with various aromatic acids in toluene at 90 °C in moderate to excellent yields. The mechanism of this tandem process was also substantiated experimentally.

Optically active amino alcohol (II) and aromatic/heteroaromatic acids give under optimized conditions exclusively or predominantly 2,4‐substituted oxazoles.

Title compounds (III) can be easily prepared under the conditions shown.