Synthesis of functionalized diarylmethanes via a copper-catalyzed cross-coupling of arylmagnesium reagents with benzylic phosphates

被引:94
作者
Kofink, Christiane C. [1 ]
Knochel, Paul [1 ]
机构
[1] Univ Munich, Dept Chem & Biochem, D-81377 Munich, Germany
关键词
DIHYDROFOLATE-REDUCTASE; ARYLBORONIC ACIDS; PNEUMOCYSTIS-CARINII; GRIGNARD-REAGENTS; MYCOBACTERIUM-AVIUM; ALLYLIC PHOSPHATES; TOXOPLASMA-GONDII; TRIMETHOPRIM; INHIBITORS; ANALOGS;
D O I
10.1021/ol0616790
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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).
引用
收藏
页码:4121 / 4124
页数:4
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