三氟甲基化
芳基
钯
组合化学
催化作用
三氟甲基
化学
氟
分子
有机化学
烷基
作者
Eun Jin Cho,Todd D. Senecal,Tom Kinzel,Yong Zhang,Donald A. Watson,Stephen L. Buchwald
出处
期刊:Science
[American Association for the Advancement of Science]
日期:2010-06-25
卷期号:328 (5986): 1679-1681
被引量:717
标识
DOI:10.1126/science.1190524
摘要
Three Fluorines at Once The trifluoromethyl (CF 3 ) group is playing an increasingly important role in the design of pharmaceutical and agrochemical compounds. CF 3 is a powerful attractor of electron density within a given molecular framework, and recently fluorine-hydrocarbon interactions have emerged as a distinct complement to the more traditional hydrophilic/hydrophobic interplay that governs docking between small molecules and proteins. Cho et al. (p. 1679 ) now present an efficient method for appending CF 3 groups to a broad range of aryl substrates. A carefully optimized palladium catalyst was able to speed up a critical elimination step that has plagued previous efforts to realize a general solution to this synthetic challenge.
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