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. 2009 Apr 2;11(7):1607-10.
doi: 10.1021/ol900298e.

Direct amination of azoles via catalytic C-H, N-H coupling

Daiki Monguchi  1 , Taiki Fujiwara, Hirotoshi Furukawa, Atsunori Mori
Affiliations

Direct amination of azoles via catalytic C-H, N-H coupling

Daiki Monguchi et al. Org Lett. .

Abstract

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.

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