Preparation of heteroaryloxetanes and heteroarylazetidines by use of a Minisci reaction.

Autor: Duncton MA; Evotec (USA), Two Corporate Drive, South San Francisco, California 94080, USA. matthew.duncton@evotec.com, Estiarte MA, Johnson RJ, Cox M, O'Mahony DJ, Edwards WT, Kelly MG
Jazyk: angličtina
Zdroj: The Journal of organic chemistry [J Org Chem] 2009 Aug 21; Vol. 74 (16), pp. 6354-7.
DOI: 10.1021/jo9010624
Abstrakt: 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.
Databáze: MEDLINE