Search Results - "Blakemore, David C"

Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes by Almond-Thynne, Joshua, Blakemore, David C, Pryde, David C, Spivey, Alan C

“…Suzuki-Miyaura cross-coupling reactions of heteroaryl polyhalides with aryl boronates are surveyed. Drawing on data from literature sources as well as bespoke…”
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Heterocyclic Allylsulfones as Latent Heteroaryl Nucleophiles in Palladium-Catalyzed Cross-Coupling Reactions by Markovic, Tim, Murray, Philip R. D, Rocke, Benjamin N, Shavnya, Andre, Blakemore, David C, Willis, Michael C

“…Heterocyclic sulfinates are effective reagents in palladium-catalyzed coupling reactions with aryl and heteroaryl halides, often providing high yields of the…”
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Iterative reactions of transient boronic acids enable sequential C–C bond formation by Battilocchio, Claudio, Feist, Florian, Hafner, Andreas, Simon, Meike, Tran, Duc N., Allwood, Daniel M., Blakemore, David C., Ley, Steven V.

“…The ability to form multiple carbon–carbon bonds in a controlled sequence and thus rapidly build molecular complexity in an iterative fashion is an important…”
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Fluorodecarboxylation for the Synthesis of Trifluoromethyl Aryl Ethers by Zhang, Qing-Wei, Brusoe, Andrew T., Mascitti, Vincent, Hesp, Kevin D., Blakemore, David C., Kohrt, Jeffrey T., Hartwig, John F.

“…The synthesis of mono‐, di‐, and trifluoromethyl aryl ethers by fluorodecarboxylation of the corresponding carboxylic acids is reported. AgF2 induces…”
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Catalyst Selection Facilitates the Use of Heterocyclic Sulfinates as General Nucleophilic Coupling Partners in Palladium-Catalyzed Coupling Reactions by Markovic, Tim, Rocke, Benjamin N., Blakemore, David C., Mascitti, Vincent, Willis, Michael C.

“…A range of 5- and 6-membered heterocycle-derived sulfinates are shown to be effective nucleophilic coupling partners with aryl chlorides and bromides using…”
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Three-Component Assembly of Multiply Substituted Homoallylic Alcohols and Amines Using a Flow Chemistry Photoreactor by Chen, Yiding, Blakemore, David C, Pasau, Patrick, Ley, Steven V

“…Oxadiazolines are bench-stable diazo precursors, which are activated under UV radiation in the presence of vinylboronic acids and aldehydes to enable a…”
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Preparation of Unsymmetrical Ketones from Tosylhydrazones and Aromatic Aldehydes via Formyl C–H Bond Insertion by Allwood, Daniel M, Blakemore, David C, Ley, Steven V

“…Preparation of ketones by insertion of diazo compounds into the formyl C–H bond of an aldehyde is an attractive procedure, but use of structurally diverse…”
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Regioselective Preparation of Saturated Spirocyclic and Ring-Expanded Fused Pyrazoles by Merchant, Rohan R, Allwood, Daniel M, Blakemore, David C, Ley, Steven V

“…Saturated bicyclic pyrazoles represent an important class of biologically active molecules, but their preparation can be hampered by labor-intensive synthesis…”
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Highly regioselective lithiation of pyridines bearing an oxetane unit by n-butyllithium by Rouquet, Guy, Blakemore, David C, Ley, Steven V

“…The first regioselective ortho-lithiation at the 4-position of simple pyridine derivatives containing a 3-oxetane unit has been achieved using n-butyllithium…”
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Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain by Bagal, Sharan K, Andrews, Mark, Bechle, Bruce M, Bian, Jianwei, Bilsland, James, Blakemore, David C, Braganza, John F, Bungay, Peter J, Corbett, Matthew S, Cronin, Ciaran N, Cui, Jingrong Jean, Dias, Rebecca, Flanagan, Neil J, Greasley, Samantha E, Grimley, Rachel, James, Kim, Johnson, Eric, Kitching, Linda, Kraus, Michelle L, McAlpine, Indrawan, Nagata, Asako, Ninkovic, Sacha, Omoto, Kiyoyuki, Scales, Stephanie, Skerratt, Sarah E, Sun, Jianmin, Tran-Dubé, Michelle, Waldron, Gareth J, Wang, Fen, Warmus, Joseph S

“…Hormones of the neurotrophin family, nerve growth factor (NGF), brain derived neurotrophic factor (BDNF), neurotrophin 3 (NT3), and neurotrophin 4 (NT4), are…”
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Selection of a novel anti-nicotine vaccine: influence of antigen design on antibody function in mice by Pryde, David C, Jones, Lyn H, Gervais, David P, Stead, David R, Blakemore, David C, Selby, Matthew D, Brown, Alan D, Coe, Jotham W, Badland, Matthew, Beal, David M, Glen, Rebecca, Wharton, Yvonne, Miller, Gavin J, White, Phil, Zhang, Ningli, Benoit, Michelle, Robertson, Karen, Merson, James R, Davis, Heather L, McCluskie, Michael J

“…Anti-nicotine vaccines may aid smoking cessation via the induction of anti-nicotine antibodies (Ab) which reduce nicotine entering the brain, and hence the…”
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Organic synthesis provides opportunities to transform drug discovery by Blakemore, David C., Castro, Luis, Churcher, Ian, Rees, David C., Thomas, Andrew W., Wilson, David M., Wood, Anthony

“…Despite decades of ground-breaking research in academia, organic synthesis is still a rate-limiting factor in drug-discovery projects. Here we present some…”
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Alkali-metal mediated zincation of N-heterocyclic substrates using the lithium zincate complex, (THF)Li(TMP)Zn( tBu) 2 and applications in in situ cross coupling reactions by Blair, Victoria L., Blakemore, David C., Hay, Duncan, Hevia, Eva, Pryde, David C.

“…This study investigates the ability of the mixed-metal reagent [Li(TMP)Zn( tBu) 2] 1 to promote direct Zn–H exchange reactions (zincations) of a wide range of…”
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A Unified Approach to Decarboxylative Halogenation of (Hetero)aryl Carboxylic Acids by Chen, Tiffany Q., Pedersen, P. Scott, Dow, Nathan W., Fayad, Remi, Hauke, Cory E., Rosko, Michael C., Danilov, Evgeny O., Blakemore, David C., Dechert-Schmitt, Anne-Marie, Knauber, Thomas, Castellano, Felix N., MacMillan, David W. C.

“…Aryl halides are a fundamental motif in synthetic chemistry, playing a critical role in metal-mediated cross-coupling reactions and serving as important…”
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Decarboxylative Borylation and Cross-Coupling of (Hetero)aryl Acids Enabled by Copper Charge Transfer Catalysis by Dow, Nathan W, Pedersen, P. Scott, Chen, Tiffany Q, Blakemore, David C, Dechert-Schmitt, Anne-Marie, Knauber, Thomas, MacMillan, David W. C

“…We report a copper-catalyzed strategy for arylboronic ester synthesis that exploits photoinduced ligand-to-metal charge transfer (LMCT) to convert…”
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One-pot three-component sulfone synthesis exploiting palladium-catalysed aryl halide aminosulfonylation by Richards-Taylor, Charlotte S, Blakemore, David C, Willis, Michael C

“…A palladium-catalysed aminosulfonylation process is used as the key-step in a one-pot, three-component sulfone synthesis. The process combines aryl-,…”
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One-Pot Synthesis of Sulfonamides from Unactivated Acids and Amines via Aromatic Decarboxylative Halosulfonylation by Pedersen, P. Scott, Blakemore, David C., Chinigo, Gary M., Knauber, Thomas, MacMillan, David W. C.

“…The coupling of carboxylic acids and amines to form amide linkages is the most commonly performed reaction in the pharmaceutical industry. Herein, we report a…”
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Pyridine sulfinates as general nucleophilic coupling partners in palladium-catalyzed cross-coupling reactions with aryl halides by Markovic, Tim, Rocke, Benjamin N, Blakemore, David C, Mascitti, Vincent, Willis, Michael C

“…Pyridine rings are ubiquitous in drug molecules; however, the pre-eminent reaction used to form carbon-carbon bonds in the pharmaceutical industry, the…”
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Photoredox Generation of Sulfonyl Radicals and Coupling with Electron Deficient Olefins by Chen, Yiding, McNamara, Nicole, May, Oliver, Pillaiyar, Thanigaimalai, Blakemore, David C, Ley, Steven V

“…Various sulfone tetrazoles were activated via iridium photoredox catalysis in the presence of DMAP to give dialkyl sulfones. The presumed sulfone radical…”
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A Photoredox Coupling Reaction of Benzylboronic Esters and Carbonyl Compounds in Batch and Flow by Chen, Yiding, May, Oliver, Blakemore, David C, Ley, Steven V

“…Mild cross-coupling reaction between benzylboronic esters with carbonyl compounds and some imines was achieved under visible-light-induced iridium-catalyzed…”
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