title: Practical synthesis of 1-aryl-6-(hydroxymethyl)-2-ketopiperazines via a 6-exo amide-epoxide cyclization.
abstract: [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.
authors.affiliation: Pfizer Global Research & Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA. noel.powell@pfizer.com
authors.forename: Noel A
authors.initials: NA
authors.lastname: Powell
authors.forename: Fred L
authors.initials: FL
authors.lastname: Ciske
authors.forename: Emma C
authors.initials: EC
authors.lastname: Clay
authors.forename: Wayne L
authors.initials: WL
authors.lastname: Cody
authors.forename: Dennis M
authors.initials: DM
authors.lastname: Downing
authors.forename: Peter G
authors.initials: PG
authors.lastname: Blazecka
authors.forename: Daniel D
authors.initials: DD
authors.lastname: Holsworth
authors.forename: Jeremy J
authors.initials: JJ
authors.lastname: Edmunds