Journal
ORGANIC LETTERS
Volume 12, Issue 4, Pages 812-815Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol902885j
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Funding
- EPSRC
- GlaxoSmithKline
- EPSRC [EP/E020607/1] Funding Source: UKRI
- Engineering and Physical Sciences Research Council [EP/E020607/1] Funding Source: researchfish
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A simple and effective method for the preparation of benzoxazolones from nitroarenes or aryl halides is described. Partial reduction of a nitro group in the presence of a chloroformate followed by a microwave-assisted rearrangement/ring closure sequence provides a convenient and practical procedure to prepare this important pharmacophore. Rearrangement precursors were also accessed from aryl halides through transition-metal-catalyzed coupling.
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