文献类型：期刊文献

中文题名：Synthesis of 1,3,5-Trisubstituted [4-tert-Butyl 2-（5,5-difluoro- 2,2-dimethyl-6-vinyl-l,3-dioxan-4-yl）acetate]pyrazoles via a Pd-Catalyzed C--H Activation

英文题名：Synthesis of 1,3,5-Trisubstituted [4-tert-Butyl 2-（5,5-difluoro- 2,2-dimethyl-6-vinyl-l,3-dioxan-4-yl）acetate]pyrazoles via a Pd-Catalyzed C--H Activation

作者：Wang Xiaoguanga[1];Fang Xiang[1];Yang Xueyana[1];Ni Meng[1];Wu Fanhong[1,2]

机构：[1]Key Laboratory for Advanced Material and Institute of Fine Chemicals, School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai 200237, China;[2]School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 200235, China

年份：2012

卷号：30

期号：12

起止页码：2767

中文期刊名：Chinese Journal of Chemistry

外文期刊名：中国化学（英文版）

收录：CSTPCD;;Scopus;CSCD:【CSCD2011_2012】；

基金：supported by the National Natural Science Foundation of China （Nos. 20972050, 21172148 and 21202044） and the Science and Technology Commission of Shanghai Municipality （No. 10540501300）.

语种：英文

中文关键词：C-H activation; Pd-catalyzed; pyrazole; HMG-CoA reductase inhibitor

外文关键词：C-H activation; Pd-catalyzed; pyrazole; HMG-CoA reductase inhibitor

摘要：The gem-difluoromethylenated acetonide 2 was efficiently synthesized as new precursor of HMG-CoA reduc- tase inhibitor. Straightforward olefination via Pd-catalyzed C4-H activation of 1,3,5-trisubstituted pyrazoles 1 was proceeded smoothly in the presence of Pd（OAc）2 and AgCO3. This protocol has merits in terms of the improved atomic economy and prevention from the generation of by-products.
The gem-difluoromethylenated acetonide 2 was efficiently synthesized as new precursor of HMG-CoA reduc- tase inhibitor. Straightforward olefination via Pd-catalyzed C4-H activation of 1,3,5-trisubstituted pyrazoles 1 was proceeded smoothly in the presence of Pd（OAc）2 and AgCO3. This protocol has merits in terms of the improved atomic economy and prevention from the generation of by-products.