Formal Dearomative Hydroamination of 2-Arylphenols
An acid-promoted dearomative rearrangement of -arylhydroxylamines affords 2-aminocyclohexadien-1-ones, which can in turn be reductively quenched for the synthesis of -aminoalcohols on a cyclohexadiene core. This method serves as an efficient entry to the pharmaceutically relevant 1-arylcyclohexylami...
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| Veröffentlicht in: | Journal of organic chemistry 2024-12 |
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| Hauptverfasser: | , , , |
| Format: | Artikel |
| Sprache: | eng |
| Online-Zugang: | Volltext |
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| Zusammenfassung: | An acid-promoted dearomative rearrangement of
-arylhydroxylamines affords 2-aminocyclohexadien-1-ones, which can in turn be reductively quenched for the synthesis of
-aminoalcohols on a cyclohexadiene core. This method serves as an efficient entry to the pharmaceutically relevant 1-arylcyclohexylamine scaffold in two steps (one purification) from commercially available or readily prepared 2-arylphenols. |
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| ISSN: | 1520-6904 1520-6904 |
| DOI: | 10.1021/acs.joc.4c02654 |