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

Direct Amination of Azoles via Catalytic C-H, N-H Coupling
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DOI:
10.1021/ol900298e
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发表时间:
2009-04-02
期刊:
影响因子:
5.2
通讯作者:
Mori, Atsunori
Mori, Atsunori
中科院分区:
化学1区
文献类型:
--
作者:
Monguchi, Daiki;Fujiwara, Taiki;Mori, Atsunori

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C-H、N-H在铜催化剂的存在下,唑与几种胺发生偶联,在2-位进行胺化。苯并噻唑与N-甲基苯胺在乙酸钠和20mol%醋酸铜(2)存在下,二甲苯中于氧气气氛下反应,得到胺化产物,产率为81%。
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.