title: Preparation of heteroaryloxetanes and heteroarylazetidines by use of a Minisci reaction.
abstract: Introduction of oxetan-3-yl and azetidin-3-yl groups into heteroaromatic bases was achieved by using a radical addition method (Minisci reaction). To demonstrate utility, the process was used to introduce an oxetane or azetidine into heteroaromatic systems that have found important uses in the drug discovery industry, such as the marketed EGFR inhibitor gefitinib, a quinolinecarbonitrile Src tyrosine kinase inhibitor, and the antimalarial hydroquinine.
authors.affiliation: Evotec (USA), Two Corporate Drive, South San Francisco, California 94080, USA. matthew.duncton@evotec.com
authors.forename: Matthew A J
authors.initials: MA
authors.lastname: Duncton
authors.forename: M Angels
authors.initials: MA
authors.lastname: Estiarte
authors.forename: Russell J
authors.initials: RJ
authors.lastname: Johnson
authors.forename: Matthew
authors.initials: M
authors.lastname: Cox
authors.forename: Donogh J R
authors.initials: DJ
authors.lastname: O'Mahony
authors.forename: William T
authors.initials: WT
authors.lastname: Edwards
authors.forename: Michael G
authors.initials: MG
authors.lastname: Kelly