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

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 mer...

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Veröffentlicht in:Chinese journal of chemistry 2012-12, Vol.30 (12), p.2767-2773
Hauptverfasser: Wang, Xiaoguang, Fang, Xiang, Yang, Xueyan, Ni, Meng, Wu, Fanhong
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Sprache:eng
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Zusammenfassung: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.
ISSN:1001-604X
1614-7065
DOI:10.1002/cjoc.201201100