Practical synthesis of 1-aryl-6-(hydroxymethyl)-2-ketopiperazines via a 6-exo amide-epoxide cyclization.

[reaction: see text] Chiral 1-aryl-6-(hydroxymethyl)-2-ketopiperazines can be prepared via an operationally simple, 6-exo epoxide ring-opening cyclization to form the ketopiperazine C6-N1 bond in high yields and with excellent enantiomeric purity.