title: Synthesis of 1- and 4-substituted piperazin-2-ones via Jocic-type reactions with N-substituted diamines.
abstract: Enantiomerically-enriched trichloromethyl-containing alcohols, obtained by asymmetric reduction, can be transformed regioselectively into 1-substituted piperazinones by modified Jocic reactions with little or no loss of stereochemical integrity. This methodology can be easily used to synthesise important pharmaceutical compounds such as the fluorobenzyl intermediate of a known PGGTase-I inhibitor.
authors.affiliation: Department of Chemistry, University of Warwick, Gibbet Hill Road, Coventry, CV4 7AL, U.K. d.j.fox@warwick.ac.uk.
authors.forename: Michael S
authors.initials: MS
authors.lastname: Perryman
authors.forename: Matthew W M
authors.initials: MW
authors.lastname: Earl
authors.forename: Sam
authors.initials: S
authors.lastname: Greatorex
authors.forename: Guy J
authors.initials: GJ
authors.lastname: Clarkson
authors.forename: David J
authors.initials: DJ
authors.lastname: Fox
mesh_terms: D003959:Diamines / Q000737:chemistry*; D054659:Diketopiperazines / Q000138:chemical synthesis* / Q000737:chemistry; D008958:Models, Molecular; D015394:Molecular Structure; D013237:Stereoisomerism
chemical_list: D003959:Diamines; D054659:Diketopiperazines