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 Fang Xiang Yang Xueyana Ni Meng Wu Fanhong 

机构地区：[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

出　　处：《Chinese Journal of Chemistry》2012年第12期2767-2773,共7页中国化学（英文版）

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）.

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.

关 键 词：C-H activation PD-CATALYZED PYRAZOLE HMG-CoA reductase inhibitor 

分 类 号：TQ252.4[化学工程—有机化工] O626.21[理学—有机化学]