文献类型：期刊文献

英文题名：Pd-Catalyzed Late-Stage Monoacetoxylation and Monoiodination of 4-Alkyl-1,5-diaryl-1H-pyrazole-3-carboxylates via Direct Csp2-H Bond Activation

作者：Fan, Xue-Min[1];Guo, Ying[1];Li, Yu-Dan[1];Yu, Kun-Kun[1];Liu, Hong-Wei[1];Liao, Dao-Hua[1];Ji, Ya-Fei[1]

机构：[1]E China Univ Sci & Technol, Sch Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China

年份：2016

卷号：5

期号：4

起止页码：499

外文期刊名：ASIAN JOURNAL OF ORGANIC CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000374772300010)，CCR-EXPANDED(收录号:WOS:000374772300010)】；

基金：We gratefully thank the National Natural Science Foundation of China ( project nos. 21176074 and 21476074) and the Research Fund for the Doctoral Program of Higher Education of China ( project no. 20130074110009) for financial support.

语种：英文

外文关键词：acetoxylation; C-H activation; iodination; palladium; pyrazoles

摘要：A palladium-catalyzed, late-stage functionalization of 4-alkyl-1,5-diaryl-1H-pyrazole-3-carboxylates to achieve acetoxylation or iodination via Csp(2)-H bond activation with synthetically useful to excellent yields is described. These straightforward transformations feature highly functionalized substrates, excellent site selectivity, rapid reaction, and simple operation. The C-O and C-I bond-forming protocols allow convenient accesses to lots of complex monoacetoxylated and monoiodinated products from pharmaceutically important intermediates. Iodoacetic acid is also used as the iodinating agent in C-H bond activation.