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Ludivine Louise‐Leriche Emilia Pǎunescu Géraldine Saint‐André Rachid Baati Anthony Romieu Alain Wagner Pierre‐Yves Renard 《Chemistry (Weinheim an der Bergstrasse, Germany)》2010,16(11):3510-3523
A new pro‐fluorescent probe aimed at a HTS assay of scavengers is able to selectively and efficiently cleave the P? S bond of organophosphorus nerve agents and by this provides non‐toxic phosphonic acid has been designed and synthesised. The previously described pro‐fluorescent probes were based on a conventional activated P? Oaryl bond cleavage, whereas our approach uses a self‐immolative linker strategy that allows the detection of phosphonothioase activity with respect to a non‐activated P? Salkyl bond. Further, we have also developed and optimised a high‐throughput screening assay for the selection of decontaminants (chemical or biochemical scavengers) that could efficiently hydrolyse highly toxic V ‐type nerve agents. A preliminary screening, realised on a small α‐nucleophile library, allowed us to identify some preliminary “hits”, among which pyridinealdoximes, α‐oxo oximes, hydroxamic acids and, less active but more original, amidoximes were the most promising. Their selective phosphonothioase activity has been further confirmed by using PhX as the substrate, and thus they offer new perspectives for the synthesis of more potent V nerve agent scavengers. 相似文献
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Ludivine Ferey Nathalie Delaunay Douglas N. Rutledge Alain Huertas Yann Raoul Pierre Gareil Jérôme Vial Isabelle Rivals 《Analytica chimica acta》2014
Because of their high toxicity, international regulatory institutions recommend monitoring specific polycyclic aromatic hydrocarbons (PAHs) in environmental and food samples. A fast, selective and sensitive method is therefore required for their quantitation in such complex samples. This article deals with the optimization, based on an experimental design strategy, of a cyclodextrin (CD) modified capillary zone electrophoresis separation method for the simultaneous separation of 19 PAHs listed as priority pollutants. First, using a central composite design, the normalized peak-start and peak-end times were modelled as functions of the factors that most affect PAH electrophoretic behavior: the concentrations of the anionic sulfobutylether-β-CD and neutral methyl-β-CD, and the percentage of MeOH in the background electrolyte. Then, to circumvent computational difficulties resulting from the changes in migration order likely to occur while varying experimental conditions, an original approach based on the systematic evaluation of the time intervals between all the possible pairs of peaks was used. Finally, a desirability analysis based on the smallest time interval between two consecutive peaks and on the overall analysis time, allowed us to achieve, for the first time in CE, full resolution of all 19 PAHs in less than 18 min. Using this optimized capillary electrophoresis method, a vegetable oil was successfully analyzed, proving its suitability for real complex sample analysis. 相似文献
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α-Fluoro-α,β-unsaturated esters 2 were efficiently synthetized via diethylzinc-promoted Wittig reaction using a phosphonium-supported triphenylphosphine SCG-PPh31, which possesses similar reactivity as its parent analog triphenylphosphine. The main advantage of this system is the use of a novel low-molecular-weight support that is soluble in solvents of medium polarities for the attachment of reagents and insoluble in solvents of low polarities. 相似文献
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Carroll L Pacheco MC Garcia L Gouverneur V 《Chemical communications (Cambridge, England)》2006,(39):4113-4115
Allenylsilanes reacted at room temperature in acetonitrile with Selectfluor, an electrophilic fluorinating reagent, to give secondary propargylic fluorides in moderate to good yields; mechanistically, a side-product resulting from a 1,2-silyl shift testifies to the presence of a cationic intermediate. 相似文献
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In this work we present an experimental apparatus devoted to the thermal characterisation of a milling tool. The experimental device used thermistors, one for each insert. Each thermistor is located at a point in the tool close to the tip of the insert. The heat flux in each insert is expressed according to the temperature at the sensor from a non-integer model. The parameters of the model are identified from transient evolutions measurements of the temperature on the sensor and on the cutting edge. An application shows the difference in the behaviour of each insert during machining from the estimated heat fluxes. To cite this article: J.-L. Battaglia et al., C. R. Mecanique 330 (2002) 857–864. 相似文献
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Potassium beta-aminoethyltrifluoroborates were prepared in good yields via hydroboration of the corresponding enecarbamates using the Snieckus hydroborating reagent. A wide variety of phenethylamines containing a potentially free primary amine after appropriate deprotection have been successfully prepared in good yield using these organotrifluoroborates as partners in Suzuki-Miyaura coupling with aryl bromides, iodides, and triflates. 相似文献
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Experimental and Theoretical Investigations of the Stereoselective Synthesis of P‐Stereogenic Phosphine Oxides
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Laurent Copey Dr. Ludivine Jean‐Gérard Dr. Eric Framery Dr. Guillaume Pilet Prof. Vincent Robert Prof. Bruno Andrioletti 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(25):9057-9061
An efficient enantioselective strategy for the synthesis of variously substituted phosphine oxides has been developed, incorporating the use of (1S,2S)‐2‐aminocyclohexanol as the chiral auxiliary. The method relies on three key steps: 1) Highly diastereoselective formation of PV oxazaphospholidine, rationalized by a theoretical study; 2) highly diastereoselective ring‐opening of the oxazaphospholidine oxide with organometallic reagents that takes place with inversion of configuration at the P atom; 3) enantioselective synthesis of phosphine oxides by cleavage of the remaining P?O bond. Interestingly, the use of a PIII phosphine precursor afforded a P‐epimer oxazaphospholidine. Hence, the two enantiomeric phosphine oxides can be synthesized starting from either a PV or a PIII phosphine precursor, which constitutes a clear advantage for the stereoselective synthesis of sterically hindered phosphine oxides. 相似文献
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Fetzer L Boff B Ali M Xiangjun M Collin JP Sirlin C Gaiddon C Pfeffer M 《Dalton transactions (Cambridge, England : 2003)》2011,40(35):8869-8878
A library of 32 organoruthenium compounds has been synthesised. Known and novel C-N cyclometalated compounds as well as N-C-N and N-N-C pincer derivatives of this metal have been used in this purpose. Most of the compounds have been tested for their in vitro antitumoral behaviours, good to excellent activities have thus been found. Several of the newly synthesized compounds pass the symbolic barrier of the nanomolar range for their IC(50) indicating a critical improvement. The level of activity is tentatively correlated to physicochemical properties of the compounds such as their Ru(III/II) redox potential and their lipophilicity (log P). 相似文献