Palladium-catalyzed direct arylation of free NH2-substituted thiophene derivatives.

Palladium-catalyzed direct arylation of free NH2-substituted thiophene derivatives.
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DOI:
10.1021/ol101758w
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发表时间:
2010-09
期刊:
影响因子:
5.2
通讯作者:
F. Derridj;J. Roger;S. Djebbar;H. Doucet
F. Derridj;J. Roger;S. Djebbar;H. Doucet
中科院分区:
化学1区
文献类型:
--
作者:
F. Derridj;J. Roger;S. Djebbar;H. Doucet

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钯催化的直接2-或5-芳基化的一些游离的NH(2)-取代的噻吩衍生物被发现在高产率进行使用各种芳基溴。在这些反应过程中,没有检测到芳基溴与噻吩NH(2)取代基的偶联。发现噻吩的C2上的酯取代基的存在可用于阻断这种高反应性碳。
The palladium-catalyzed direct 2- or 5-arylation of some free NH(2)-substituted thiophene derivatives was found to proceed in high yields using a variety of aryl bromides. In the course of these reactions, no coupling of the aryl bromide with the thiophene NH(2) substituent was detected. The presence of an ester substituent on C2 of thiophene was found to be useful to block this highly reactive carbon.