Preparation of heteroaryloxetanes and heteroarylazetidines by use of a Minisci reaction.
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.
Duncton
Matthew A J
MA
Evotec (USA), Two Corporate Drive, South San Francisco, California 94080, USA. matthew.duncton@evotec.com
Estiarte
M Angels
MA
Johnson
Russell J
RJ
Cox
Matthew
M
O'Mahony
Donogh J R
DJ
Edwards
William T
WT
Kelly
Michael G
MG