钯催化的杂芳基溴化物、碘化物、三氟甲磺酸酯和芳基碘化物的二氟甲基硫醇化反应。

Wu Jiang, Liu Yafei, Lu Changhui, Shen Qilong

Key Laboratory of Organofluorine Chemistry , Shanghai Institute of Organic Chemistry , Chinese Academy of Sciences , 345 Lingling Road , Shanghai 200032 , China . Email:

Chem Sci. 2016 Jun 1;7(6):3757-3762. doi: 10.1039/c6sc00082g. Epub 2016 Feb 17.

A palladium-catalyzed difluoromethylthiolation of heteroaryl halides and triflates under mild conditions was described. A vast range of heteroaryl halides such as pyridyl, quinolinyl, benzothiazolyl, thiophenyl, carbazolyl and pyazolyl halides could be difluoromethylthiolated efficiently, thus providing medicinal chemists with new tools for their search of new lead compounds for drug discovery. Likewise, aryl iodides were difluoromethylthiolated in high yields under a modified reaction condition.

描述了在温和条件下钯催化的杂芳基卤化物和三氟甲磺酸酯的二氟甲基硫醇化反应。多种杂芳基卤化物，如吡啶基、喹啉基、苯并噻唑基、噻吩基、咔唑基和吡唑基卤化物，都能有效地进行二氟甲基硫醇化反应，从而为药物化学家寻找用于药物发现的新先导化合物提供了新工具。同样，在改进的反应条件下，芳基碘化物也能以高产率进行二氟甲基硫醇化反应。