Synthesis of functionalized diarylmethanes via a copper-catalyzed cross-coupling of arylmagnesium reagents with benzylic phosphates
Synthesis of functionalized diarylmethanes via a copper-catalyzed cross-coupling of arylmagnesium reagents with benzylic phosphates
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DOI：
10.1021/ol0616790
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发表时间：
2006-08-31
期刊：
影响因子：
5.2
通讯作者：
Knochel, Paul
中科院分区：
文献类型：
--
作者：
Kofink, Christiane C.;Knochel, Paul
氯化铜、亚磷酸三乙酯和碘化四丁基铵的组合是使用芳基卤化镁与苄基磷酸盐的交叉偶联反应合成多官能化二芳基甲烷的非常有效的催化体系。抗生素甲氧苄啶已经使用这种Cu（I）催化的交叉偶联以52%的总产率（四步）制备。
A combination of copper chloride, triethyl phosphite, and tetrabutylammonium iodide is a very efficient catalytic system for the synthesis of polyfunctionalized diarylmethanes, using the cross-coupling reaction of arylmagnesium halides with benzylic phosphates. The antibiotic Trimethoprim has been prepared using this Cu(I)-catalyzed cross-coupling in 52% overall yield (four steps).