Journal ArticleDOI
From 2000 to mid-2010: a fruitful decade for the synthesis of pyrazoles.
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This article is published in Chemical Reviews.The article was published on 2011-08-01. It has received 839 citations till now.read more
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Use of a Traceless Activating and Directing Group for the Construction of Trifluoromethylpyrazoles: One-Pot Transformation of Nitroolefins and Trifluorodiazoethane.
Zhen Chen,Yan Zheng,Jun-An Ma +2 more
TL;DR: This method takes advantage of the nitro group as a traceless activating and directing group (TADG) that is released in the aromatization step to produce 4-substituted 3-perfluoroalkyl pyrazoles with complete regioselectivity.
Journal ArticleDOI
Enantioselective Synthesis of Dihydrospiro[indoline-3,4'-pyrano[2,3-c]pyrazole] Derivatives via Michael/Hemiketalization Reaction.
TL;DR: A new bifunctional squaramide organocatalyst derived from L-proline mediated the first enantioselective synthesis of dihydrospiro[indoline-3,4'-pyrano[2,3-c]pyrazole] derivatives in excellent enantiOSElectivity by reacting pyrazolones with isatylidine β,γ-unsaturated α-ketoester.
Journal ArticleDOI
Organocatalytic one-pot asymmetric synthesis of 4H,5H-pyrano[2,3-c]pyrazoles.
TL;DR: An efficient one pot asymmetric synthesis of tetrahydropyrano[2,3-c]pyrazoles has been developed and the title compounds were accessible in good to very good yields and very good to excellent enantioselectivities after a single purification step.
Journal ArticleDOI
Enantioselective synthesis of functionalized pyrazoles by NHC-catalyzed reaction of pyrazolones with α,β-unsaturated aldehydes.
TL;DR: The N-heterocyclic carbene (NHC)-organocatalyzed enantioselective annulation reaction of pyrazolones with α,β-unsaturated aldehydes proceeding via the chiral α, β-uns saturated acyl azolium intermediates under oxidative conditions is presented.
Journal ArticleDOI
Intermolecular Palladium(0)-Catalyzed Atropo-enantioselective C–H Arylation of Heteroarenes
TL;DR: An intermolecular and highly enantioselective C-H arylation of relevant heteroarenes providing an efficient access to atropisomeric (hetero)biaryls is reported.
References
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Journal ArticleDOI
Recent developments in isocyanide based multicomponent reactions in applied chemistry
Journal ArticleDOI
Modern Synthetic Methods for Copper‐Mediated C(aryl) ? O, C(aryl) ? N, and C(aryl) ? S Bond Formation
Steven V. Ley,Andrew Thomas +1 more
TL;DR: In this article, the authors highlight the recent developments in the copper-mediated (both stoichiometric and catalytic) reactions of aryl boronic acids as reaction partners in both O- and N-arylation.
Journal ArticleDOI
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
T. D. Penning,John J. Talley,Bertenshaw,Jeffery S. Carter,P. W. Collins,Stephen H. Docter,Matthew J. Graneto,Len F. Lee,James W. Malecha,Julie M. Miyashiro,Roland S. Rogers,D. J. Rogier,Stella S. Yu,AndersonGD,E. G. Burton,J. N. Cogburn,Susan A. Gregory,Carol M. Koboldt,W E Perkins,Karen Seibert,A. W. Veenhuizen,Yan Y. Zhang,P. C. Isakson +22 more
TL;DR: 1i (4-[5-(4-methylphenyl)-3-(trifluoromethyl)- H-pyrazol-1-yl]benzenesulfonamide, SC-58635, celecoxib), which is currently in phase III clinical trials for the treatment of rheumatoid arthritis and osteoarthritis, is identified.
Journal ArticleDOI
Copper-mediated coupling reactions and their applications in natural products and designed biomolecules synthesis.
TL;DR: Using R-Hydroxy Stannanes as a Model for a Methylenation Reaction and Conclusions and Future Prospects are presented.
BookDOI
Synthetic applications of 1,3-dipolar cycloaddition chemistry toward heterocycles and natural products
Albert Padwa,William H. Pearson +1 more
TL;DR: In this paper, the authors present a list of the most important properties of Nitrones and Azomethine Ylides: Nitrones (Jason N. Martin and Raymond C. Jones), Nitronates (Scott E. Denmark and Jeromy J. Cottell), Azides (Chin-Kang Sha and A. K. Mohanakrishnan). Mesoionic Ring Systems (Gordon W. Gribble). Effect of External Reagents (Shuji Kanemasa). Asymmetric Reactions (Kurt Vesterager Gothe
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Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
T. D. Penning,John J. Talley,Bertenshaw,Jeffery S. Carter,P. W. Collins,Stephen H. Docter,Matthew J. Graneto,Len F. Lee,James W. Malecha,Julie M. Miyashiro,Roland S. Rogers,D. J. Rogier,Stella S. Yu,AndersonGD,E. G. Burton,J. N. Cogburn,Susan A. Gregory,Carol M. Koboldt,W E Perkins,Karen Seibert,A. W. Veenhuizen,Yan Y. Zhang,P. C. Isakson +22 more