Department of Chemistry, Tongji University, Siping Road 1239, Shanghai 200092, China.
Beilstein J Org Chem. 2011;7:1656-62. doi: 10.3762/bjoc.7.195. Epub 2011 Dec 12.
An efficient synthesis of 1,3-diaryl-4-halo-1H-pyrazoles was achieved. The synthesis involves the [3 + 2] dipolar cycloaddition of 3-arylsydnones and 2-aryl-1,1-dihalo-1-alkenes. The process proceeds smoothly in moderate to excellent yields. 1,3-Diaryl-4-halo-1H-pyrazoles are found to be important intermediates that can easily be converted into 1,2,5-triaryl-substituted pyrazoles via Pd-catalyzed C-H bond activation.
1,3-二芳基-4-卤代-1H-吡唑的高效合成方法。该合成方法涉及 3-芳基丁二酮和 2-芳基-1,1-二卤代-1-烯烃的[3+2]偶极环加成反应。该过程在中等至优异的收率下顺利进行。1,3-二芳基-4-卤代-1H-吡唑是重要的中间体，通过 Pd 催化的 C-H 键活化可以很容易地转化为 1,2,5-三芳基取代的吡唑。
