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544 results on '"Linclau, Bruno"'

151. The Synthesis and in vivo Evaluation of 2′,2′-Difluoro KRN7000

Author

Leung, Leo, primary, Tomassi, Cyrille, additional, Van Beneden, Katrien, additional, Decruy, Tine, additional, Trappeniers, Matthias, additional, Elewaut, Dirk, additional, Gao, Yifang, additional, Elliott, Tim, additional, Al-Shamkhani, Aymen, additional, Ottensmeier, Christian, additional, Werner, Jörn M., additional, Williams, Anthony, additional, Van Calenbergh, Serge, additional, and Linclau, Bruno, additional

Published
2009
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157. Synthesis and In Vivo Evaluation of 4-Deoxy-4,4-difluoro-KRN7000

Author

Leung, Leo, primary, Tomassi, Cyrille, additional, Van Beneden, Katrien, additional, Decruy, Tine, additional, Elewaut, Dirk, additional, Elliott, Tim, additional, Al-Shamkhani, Aymen, additional, Ottensmeier, Christian, additional, Van Calenbergh, Serge, additional, Werner, Joern, additional, Williams, Tony, additional, and Linclau, Bruno, additional

Published
2008
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159. Synthesis and in vitro Evaluation of α‐GalCer Epimers

Author

Trappeniers, Matthias, primary, Goormans, Stijn, additional, Van Beneden, Katrien, additional, Decruy, Tine, additional, Linclau, Bruno, additional, Al‐Shamkhani, Aymen, additional, Elliott, Tim, additional, Ottensmeier, Christian, additional, Werner, Joern M., additional, Elewaut, Dirk, additional, and Van Calenbergh, Serge, additional

Published
2008
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163. A Computational Study of Vicinal Fluorination in 2,3-Difluorobutane: Implications for Conformational Control in Alkane Chains.

Author

Fox, Stephen J., Gourdain, Stephanie, Coulthurst, Anton, Fox, Clare, Kuprov, Ilya, Essex, Jonathan W., Skylaris, Chris ‐ Kriton, and Linclau, Bruno

Subjects
FLUORINATION, DIASTEREOISOMERS, CONFORMATIONAL analysis, DENSITY functional theory, LANGMUIR isotherms
Abstract

A comprehensive conformational analysis of both 2,3-difluorobutane diastereomers is presented based on density functional theory calculations in vacuum and in solution, as well as NMR experiments in solution. While for 1,2-difluoroethane the fluorine gauche effect is clearly the dominant effect determining its conformation, it was found that for 2,3-difluorobutane there is a complex interplay of several effects, which are of similar magnitude but often of opposite sign. As a result, unexpected deviations in dihedral angles, relative conformational energies and populations are observed which cannot be rationalised only by chemical intuition. Furthermore, it was found that it is important to consider the free energies of the various conformers, as these lead to qualitatively different results both in vacuum and in solvent, when compared to calculations based only on the electronic energies. In contrast to expectations, it was found that vicinal syn-difluoride introduction in the butane and by extension, longer hydrocarbon chains, is not expected to lead to an effective stabilisation of the linear conformation. Our findings have implications for the use of the vicinal difluoride motif for conformational control. [ABSTRACT FROM AUTHOR]

Published
2015
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181. Synthesis of Heterocycles Using Polymer-Supported Reagents under Microwave Irradiation.

Author

Eycken, Erik, Kappe, C. Oliver, Crosignani, Stefano, and Linclau, Bruno

Abstract

In this chapter, the microwave-assisted synthesis of heterocyclic systems using polymer-supported reagents is reviewed. After a brief introduction on the advantages of using polymer-supported reagents under microwave irradiation, a survey of the current literature on the field is given, highlighting whenever possible the differences in behavior when compared to the same reactions performed with conventional heating. The chapter will focus on the use of dedicated monomode microwave systems and on reactions run in the presence of solvents and involving either polymer-supported reagents, catalysts or scavengers. Reactions run in the absence of solvents, with the reagents impregnated on various kinds of supports, will not be included. [ABSTRACT FROM AUTHOR]

Published
2006
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187. Tetrafluorination of Sugars as Strategy for Enhancing Protein-Carbohydrate Affinity: Application to UDP-Gal p Mutase Inhibition.

Author

N'Go, Inès, Golten, Samuel, Ardá, Ana, Cañada, Javier, Jiménez‐Barbero, Jesús, Linclau, Bruno, and Vincent, Stéphane P.

Subjects
UDP-galactopyranose mutase, PROTEIN-carbohydrate interactions, FLUORINATION, MYCOBACTERIUM tuberculosis, BACTERIAL cell walls, BACTERIAL enzymes, NUCLEAR magnetic resonance
Abstract

Tetrafluorinated analogues of both UDP-galactopyranose and UDP-galactofuranose have been synthesized and assayed against UDP-galactopyranose mutase, a key enzyme for Mycobacterium tuberculosis cell wall biosynthesis. Competition assays and STD-NMR spectroscopy techniques have evidenced not only the first unambiguous case of affinity enhancement through local sugar polyfluorination, but also showed that tetrafluorination can still have a beneficial effect on binding when monofluorination at the same position does not. [ABSTRACT FROM AUTHOR]

Published
2014
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188. Additions and corrections

Author

Linclau, Bruno, Singh, Ashvani K., and Curran, Dennis P.

Subjects
Amines -- Research, Organic compounds -- Synthesis, Solution (Chemistry) -- Research, Biological sciences, Chemistry
Published
1999

193. The conformation of tetrafluorinated methyl galactoside anomers: crystallographic and NMR studies

Author

Linclau, Bruno, Golten, Samuel, Light, Mark, Sebban, Muriel, and Oulyadi, Hassan

Subjects
*FLUORINATION, *GLYCOSIDES, *CRYSTALLOGRAPHY, *X-ray diffraction, *MONOSACCHARIDES, *FLUORINE, *NUCLEAR magnetic resonance
Abstract

Abstract: The first single-crystal X-ray diffraction study of tetrafluorinated monosaccharide derivatives is presented. Both α- and β-methyl 2,3-dideoxy-2,2,3,3-tetrafluoro-d-galactopyranoside anomers adopt the 4 C 1 conformation. The values for the C1–O1 and C1–O5 bond lengths and the O5–C1–O1–CH3 dihedral angles are in line with what can be expected from the anomeric and exo-anomeric effects. The chair conformations are slightly distorted, presumably due to repulsion between 1,3-diaxial C–O and C–F bonds. The asymmetric unit of both compounds contains up to three independent molecules, which differ in the conformation of the hydroxymethyl group (including in one case a ‘forbidden’gg rotamer). The molecular packing of the β-anomer shows a clear segregation between fluorinated and hydrophilic domains, while for the α-anomer the regions of fluorine segregation are broken by interleafing of OMe groups. There is one close OH⋯F contact, which is likely to arise from the crystal packing. NMR studies show that the two anomers also adopt a 4 C 1 conformation in solution (D2O, CDCl3). [Copyright &y& Elsevier]

Published
2011
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194. A convenient AIBN-initiated radical addition of ethyl iododifluoroacetate to alkenes

Author

Leung, Leo and Linclau, Bruno

Subjects
*ORGANIC chemistry, *ETHYL acetoacetate, *CHROMOGENIC compounds, *ALKENES
Abstract

Abstract: The AIBN-initiated addition of ethyl 4-iodo-2,2-difluoroacetate to a variety of alkene substrates is described. The addition generally led to the corresponding addition products in good to excellent yields and various functional groups could be tolerated under the reaction conditions. [Copyright &y& Elsevier]

Published
2008
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196. Microwaves, supported-reagents and parallel synthesis: Isocyanide and ester synthesis.

Author

Crosignani, Stefano, Launay, Delphine, Linclau, Bruno, and Bradley, Mark

Abstract

The benefits of microwave irradiation are described for a numberof important reactions such as amid and ester formation anddehydration of formamide to the corresponding isonitriles. Notonly were reaction times dramatically reduced but thetransformations were less prone to side reactions anddecomposition. [ABSTRACT FROM AUTHOR]

Published
2003
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198. Efficient Desymmetrization of 'Pseudo'-C[sub 2]-Symmetric Substrates: Illustration in the Synthesis of a Disubstituted Butenolide from Arabitol.

Author

Linclau, Bruno, Boydell, A. James, Clarke, Philip J., Horan, Richard, and Jacquet, Claire

Subjects
*RING formation (Chemistry), *ORGANIC chemistry
Abstract

A short synthesis of the homochiral disubstituted butenolide 1 is described in four steps from arabitol. The key steps are the selective kinetic protection of arabitol and the cyclization of 11 to form the butenolide ring. This last transformation represents a rare example of a fully stereoselective cyclitive desymmetrization process of a "pseudo"-C[sub 2]-symmetric substrate. [ABSTRACT FROM AUTHOR]

Published
2003
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199. Cover Feature: Cubane Electrochemistry: Direct Conversion of Cubane Carboxylic Acids to Alkoxy Cubanes Using the Hofer–Moest Reaction under Flow Conditions (Chem. Eur. J. 2/2020).

Author

Collin, Diego E., Folgueiras‐Amador, Ana A., Pletcher, Derek, Light, Mark E., Linclau, Bruno, and Brown, Richard C. D.

Subjects
CARBOXYLIC acids, CUBANES, ELECTROCHEMISTRY, FLOW chemistry, ELECTROSYNTHESIS
Abstract

Cover Feature: Cubane Electrochemistry: Direct Conversion of Cubane Carboxylic Acids to Alkoxy Cubanes Using the Hofer-Moest Reaction under Flow Conditions (Chem. Eur. J. 2/2020) The possibility of using electrochemical methods to transform cubane carboxylic acids presented an intriguing possibility, leading to the development of anodic decarboxylative ether formation in flow. Bioisostere, cubanes, electrosynthesis, flow electrochemistry, oxidative decarboxylation. [Extracted from the article]

Published
2020
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200. Rapid Screening of Diverse Biotransformations for Enzyme Evolution

Author

Kempa, Emily E., Galman, James L., Parmeggiani, Fabio, Marshall, James R., Malassis, Julien, Fontenelle, Clement Q., Vendeville, Jean-Baptiste, Linclau, Bruno, Charnock, Simon J., Flitsch, Sabine L., Turner, Nicholas J., and Barran, Perdita E.

Abstract

The lack of label-free high-throughput screening technologies presents a major bottleneck in the identification of active and selective biocatalysts, with the number of variants often exceeding the capacity of traditional analytical platforms to assess their activity in a practical time scale. Here, we show the application of direct infusion of biotransformations to the mass spectrometer (DiBT-MS) screening to a variety of enzymes, in different formats, achieving sample throughputs equivalent to ∼40 s per sample. The heat map output allows rapid selection of active enzymes within 96-well plates facilitating identification of industrially relevant biocatalysts. This DiBT-MS screening workflow has been applied to the directed evolution of a phenylalanine ammonia lyase (PAL) as a case study, enhancing its activity toward electron-rich cinnamic acid derivatives which are relevant to lignocellulosic biomass degradation. Additional benefits of the screening platform include the discovery of biocatalysts (kinases, imine reductases) with novel activities and the incorporation of ion mobility technology for the identification of product hits with increased confidence.

Published
2021
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