Department of Process Research and Development, Merck & Co., Inc., Rahway, NJ, USA.
Angew Chem Int Ed Engl. 2017 Apr 10;56(16):4478-4482. doi: 10.1002/anie.201700244. Epub 2017 Mar 24.
The conversion of aryl halides to phenols under mild reaction conditions is a longstanding and formidable challenge in organic chemistry. Herein, we report the rational design of a broadly applicable Pd-catalyzed method to prepare phenols with benzaldehyde oxime as a hydroxide surrogate. These reactions occur under mildly basic conditions and enable the late-stage hydroxylation of several functionally-dense drug-like aryl halides.
在温和的反应条件下将芳基卤化物转化为酚类化合物是有机化学中长期存在的难题。在此，我们报告了一种广泛适用的钯催化方法的合理设计，该方法使用苯甲醛肟作为氢氧根替代物来制备酚类化合物。这些反应在弱碱性条件下进行，并能实现几种功能密集型药物样芳基卤化物的后期羟化。
