Direct Amination of Azoles via Catalytic C−H, N−H Coupling

Direct Amination of Azoles via Catalytic C−H, N−H Coupling

C−H, N−H Coupling of azoles takes place with several amines in the presence of a copper catalyst to undergo amination at the 2-position. The reaction of benzothiazole with N-methylaniline in the presence of sodium acetate and 20 mol % Cu(OAc)2 in xylene under an oxygen atmosphere afforded the aminat...

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Veröffentlicht in:Organic letters 2009-04, Vol.11 (7), p.1607-1610
Hauptverfasser: Monguchi, Daiki, Fujiwara, Taiki, Furukawa, Hirotoshi, Mori, Atsunori
Format: Artikel
Sprache:eng
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Zusammenfassung:C−H, N−H Coupling of azoles takes place with several amines in the presence of a copper catalyst to undergo amination at the 2-position. The reaction of benzothiazole with N-methylaniline in the presence of sodium acetate and 20 mol % Cu(OAc)2 in xylene under an oxygen atmosphere afforded the aminated product in 81% yield.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol900298e