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排序方式: 共有118条查询结果,搜索用时 15 毫秒
31.
F. Valensi N. Pellerin S. Pellerin Q. Castillon K. Dzierzega F. Briand J.-P. Planckaert 《Plasma Chemistry and Plasma Processing》2018,38(1):177-205
Metal Active Gas (MAG) welding in presence of Argon and CO2 mixture as shielding gas is a largely developed process allowing the transfer of the liquid metal from the consumable wire anode to the workpiece according to various modes (short-arc, globular, spray-arc). The CO2 presence in the shielding gas leads to the formation of an oxide layer, or gangue, wrapping the droplet, limiting the access to the spray-mode transfer, taking into account the low conductivity and the high viscosity of this layer. Several electrodes of various compositions have been tested thanks to Flux Cored Arc Welding, to limit the gangue formation or its negative contribution, based on Ti, La, Zr and alkali metals addition or reduction in silicon content. The results are interpreted considering the metal transfer mode for a given current intensity (330 and 410 A), with various CO2 concentrations in the shielding gas. Finally, the role of the gangue, compared to the other factors governing the droplet detachment, is discussed. A decrease in silicon content limits significantly the gangue formation and gives access to spray arc transfer up to 30 vol.% of CO2 at 330 A. Titanium addition leads to the same results. The tests in presence of zirconium proved the conductivity improvement of the gangue. The addition of alkali allows to stabilize the spray arc up to the noteworthy value of 60 vol.% of CO2 at 330 A, supporting the hypothesis of a strong influence of viscosity on droplets detachment in the process. 相似文献
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Bianco A Furrer J Limal D Guichard G Elbayed K Raya J Piotto M Briand JP 《Journal of combinatorial chemistry》2000,2(6):681-690
The solid-phase synthesis of 2,5-diketopiperazines containing the trans-4-hydroxy-L-proline amino acid residue (Hyp) was performed on Ellman polystyrene, polyoxyethylene-polyoxypropylene (POEPOP), polystyrene-polyoxyethylene NovaSyn, and Wang resins, respectively. The reaction pathway allowed the introduction of different functional groups around the bicyclic scaffold in a combinatorial approach, and it generated mixtures of isomers. A detailed characterization of the single reaction steps by high resolution magic angle spinning (HRMAS) NMR spectroscopy was performed. The NMR spectral resolution of the resin-bound intermediates and final products was greatly influenced by the polymer matrix. The POEPOP resin permitted to obtain HRMAS NMR spectra with a resolution comparable with that of the spectra of the molecules in solution. Moreover, configurational and conformational isomers formed during the solid-phase reaction steps could be detected and easily assigned. Therefore, the combination of the HRMAS NMR technique with the use of nonaromatic resins may become an extremely powerful tool in solid-phase organic synthesis. This approach will allow the monitoring of multistep reactions and the conception of on-bead structural studies either on small molecules or on natural and/or synthetic oligomers. 相似文献
34.
A new, efficient, and readily available reagent, methyl 2-((succinimidooxy)carbonyl)benzoate (MSB), for N-phthaloylation of amino acids and amino acid derivatives is described. The phthaloylation procedure is simple and racemization-free and gives excellent results with alpha-amino acids, alpha-amino alcohols, dipeptides, alpha-amino carboxamides, and alpha-amino esters. 相似文献
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36.
Solid-phase synthesis of fullerene-peptides 总被引:1,自引:0,他引:1
Pantarotto D Bianco A Pellarini F Tossi A Giangaspero A Zelezetsky I Briand JP Prato M 《Journal of the American Chemical Society》2002,124(42):12543-12549
The solid-phase synthesis of peptides (SPPS) containing [60]fullerene-functionalized amino acids is reported. A new amino acid, fulleropyrrolidino-glutamic acid (Fgu), is used for the SPPS of a series of analogues of different length based on the natural Leu(5)-Enkephalin and on cationic antimicrobial peptides. These fullero-peptides were prepared on different solid supports to analyze the influence of the resin on the synthesis. Optimized protocols for the coupling and deprotection procedures were determined allowing the synthesis of highly pure peptides in sufficient quantities for evaluation of biological activities. In particular, to avoid side reactions of the fullerene moiety with bases and nucleophiles, the removal of the protecting groups was performed under inert conditions (nitrogen or argon in the dark). We have encountered serious problems with the recovery of the crude compounds, especially when Fgu was inserted in the proximity of the resin core as fullero-peptides tend to remain embedded inside the resin. Eventually, all of the fullero-peptides were easily purified, and the cationic peptides were tested for their antimicrobial activities. They displayed a specific activity against the Gram-positive bacterium S. aureus and also lysed erythrocytes. The availability of a fullero-amino acid easily useable in the SPPS of fullero-peptides may thus open the way to the synthesis of new types of biologically active oligomers. 相似文献
37.
Marin J Didierjean C Aubry A Briand JP Guichard G 《The Journal of organic chemistry》2002,67(24):8440-8449
The synthesis of (2S,5R)-5-hydroxy-6-oxo-1,2-piperidinedicarboxylates (5) and related (3S,6R)-3-hydroxy-6-alkyl-2-oxo-1-piperidinecarboxylates has been developed. The approach is based on the asymmetric hydroxylation of enolates generated from the corresponding N-protected-6-substituted piperidin-2-ones. The utility of 5a as a precursor in the synthesis of (2S,5R)-5-hydroxylysine (1), an amino acid unique to collagen and collagen-like proteins, has also been demonstrated. (2S)-6-oxo-1,2-piperidinedicarboxylates (6) required for hydroxylation studies were prepared in 38-74% yield, starting from conveniently protected aspartic acid as inexpensive chiral adduct. Hydroxylation of 6 to 5 proceeds in high yield and excellent diastereoselectivity by treatment of their Li-enolate with (+)-camphorsulfonyloxaziridine at -78 degrees C. Ring opening of di-tert-butyl (2S,5R)-6-oxo-1,2-piperidinedicarboxylate ((5R)-5a) under reductive conditions afforded the corresponding 1,2-diol (17) in 91%, which was further transformed to (2S,5R)-5-hydroxylysine in four steps (84%). 17 is also a versatile intermediate in the preparation of tert-butyl (2S,5R)-2-[(tert-butoxycarbonyl)amino]-5-hydroxy-6-iodohexanoate (3) and tert-butyl (2S)-2-[(tert-butoxycarbonyl)amino]-4-[(2R)-oxiranyl]butanoate (4), two amino acid derivatives used in the total synthesis of the bone collagen cross-link (+)-pyridinoline (2a). 相似文献
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39.
Lena G Lallemand E Gruner AC Boeglin J Roussel S Schaffner AP Aubry A Franetich JF Mazier D Landau I Briand JP Didierjean C Rénia L Guichard G 《Chemistry (Weinheim an der Bergstrasse, Germany)》2006,12(33):8498-8512
The development of the 1,3,5-triazepane-2,6-dione system as a novel, conformationally restricted, and readily accessible class of dipeptidomimetics is reported. The synthesis of the densely functionalized 1,3,5-triazepane-2,6-dione skeleton was achieved in only four steps from a variety of simple linear dipeptide precursors. To extend the practical value of 1,3,5-triazepane-2,6-diones, a general polymer-assisted solution-phase synthesis approach amenable to library production in a multiparallel format was developed. The conformational preferences of the 1,3,5-triazepane-2,6-dione skeleton were investigated in detail by NMR spectroscopy and X-ray diffraction. The ring exhibits a characteristic folded conformation which was compared to that of related dipeptide-derived scaffolds including the more planar 2,5-diketopiperazine (DKP). Molecular and structural diversity was increased further through post-cyclization appending operations at urea nitrogens. Preliminary biological screens of a small collection of 1,3,5-triazepane-2,6-diones revealed inhibitors of the underexplored malaria liver stage and suggest strong potential for this dipeptide-derived scaffold to interfere with and to modulate biological pathways. 相似文献
40.
Pastorin G Marchesan S Hoebeke J Da Ros T Ehret-Sabatier L Briand JP Prato M Bianco A 《Organic & biomolecular chemistry》2006,4(13):2556-2562
Four different regioisomers of cationic bis-N,N-dimethylfulleropyrrolidinium salts have been prepared and evaluated as inhibitors of the enzymatic activity of acetylcholinesterase. These fullerene-based derivatives were found to be noncompetitive inhibitors of acetylthiocholine hydrolysis. Molecular modelling was used to describe the possible interactions between the fullerene cage and the amino acids surrounding the cavity of the enzyme. The cationic C(60) derivatives used in this study represent a new class of molecules potentially able to modulate the enzymatic activity of acetylcholinesterase. 相似文献