Search results for "Esters"
showing 10 items of 305 documents
ChemInform Abstract: Aza-Henry Reaction of Isatin Ketimines with Methyl 4-Nitrobutyrate en Route to Spiro[piperidine-3,3′-oxindoles].
2016
A new enantioselective route to spiro[piperidine-3,3′-oxindoles] from isatin ketimines is described. The aza-Henry reaction of N-Boc-isatin ketimines with methyl 4-nitrobutyrate in the presence of a Ph2BOX-CuBr2 complex provided the corresponding nitro amino esters with good diastereoselectivity and excellent enantioselectivity (up to >99% ee). The aza-Henry adducts were transformed into spiro[piperidine-3,3′-oxindoles] after reduction of the nitro group to oxime, and cleavage of the N-Boc group and lactamisation.
Aza-Henry Reaction of Isatin Ketimines with Methyl 4-Nitrobutyrate en Route to Spiro[piperidine-3,3′-oxindoles]
2015
A new enantioselective route to spiro[piperidine-3,3′-oxindoles] from isatin ketimines is described. The aza-Henry reaction of N-Boc-isatin ketimines with methyl 4-nitrobutyrate in the presence of a Ph2BOX-CuBr2 complex provided the corresponding nitro amino esters with good diastereoselectivity and excellent enantioselectivity (up to >99% ee). The aza-Henry adducts were transformed into spiro[piperidine-3,3′-oxindoles] after reduction of the nitro group to oxime, and cleavage of the N-Boc group and lactamisation.
ChemInform Abstract: Synthesis and Stereochemical Studies of 2-Substituted Thiazolidine-4-carboxamide Derivatives.
2010
A series of new 2-substituted thiazolidine-4-carboxamide derivatives which have potentially useful immunological properties, have been synthesized in a stereoselective manner by coupling 2-subsituted thiazolidine-4-carboxylic acids with amines or amino esters. The structure of these compounds was established by combination of NMR methods and by X-ray analysis.
Pharmakologisch aktive polymere, 8.Poly[2-(methylsulfinyl)äthylacrylat]e und ihre vermittelnde wirkung auf die transkutane resorption von pharmaka
1975
Poly[2-(methylsulfinyl)athylacrylat] (2a) und Poly[2-(methylsulfinyl)athylmethacrylat] (2b) wurden synthetisiert und auf ihre vermittelnde Wirkung bei transkutaner Resorption einiger Pharmaka untersucht. 2b verbesserte die Resorption der Phosphorsaureester Dimethoat® und Paraoxon® und der p-Aminohippursaure und war etwa mit der Wirksamkeit von DMSO vergleichbar. Ein geringer penetrationsfordernder Effekt ergab sich fur Dinitrochlorbenzol. Nicht beeinflust wurde die dermale Resorption von Isoprenalinsulfat. Die beiden Polymeren zeigten eine gute Lokalvertraglichkeit und 2b auch keine akute Allgemeintoxizitat bei systematischer Anwendung. Der fur DMSO charakteristische knoblauchartige Geruch …
Single- and Double-Strand Breaks of Dry DNA Exposed to Protons at Bragg-Peak Energies
2017
International audience; Ultrathin layers (<20 nm) of pBR322 plasmid DNA were deposited onto 2.5 μm thick polyester films and exposed to proton Bragg-peak energies (90–3000 keV) at various fluences. A quantitative analysis of radio-induced DNA damage is reported here in terms of single- and double-strand breaks (SSB and DSB, respectively). The corresponding yields as well as G-values and the cross sections exhibit fairly good agreement with the rare available data, stemming from close experimental conditions, namely, based on α particle irradiation. SSB/DSB rates appear to be linear when plotted against linear energy transfer (LET) in the whole energy range studied. All the data present a ma…
Recovery of aliphatic low-molecular-mass carboxylic acids from hardwood kraft black liquor
2015
Abstract During alkaline pulping of wood, substantial amounts of carbohydrates-derived aliphatic carboxylic acids (formic and acetic acids together with various hydroxy acids) are formed and dissolved into the cooking liquor (“black liquor”). These acids with low heating values are considered to be potential feedstocks for the chemical industry but, due to many factors, their straightforward recovery as free acids from black liquor (pH 13–14) is difficult. In this paper, we outlined the partial recovery of volatile formic and acetic acids from the acidified birch ( Betula pendula ) kraft black liquor (pH approximately 2.5) by distillation, and the partial recovery of significant low-molecul…
Mixtures of lecithin with polymerizable derivatives of cholesterol. A monolayer film balance study.
1986
One of the best investigated binary lipid mixtures is the lecithin-cholesterol system. We show here that it is possible to modify the cholesterol in such a way that it can be polymerized without changing its behaviour in mixtures with lecithin. The polymerizable derivatives exhibit a very similar phase diagram in the mixture with dipalmitoyl-phosphatidylcholine as the cholesterol itself. This is demonstrated by filmbalance measurements.
Regulation of the activity of the Cholesteryl Ester Tranfer Protein (CETP) : electrostatics interactions with carboxylic derivatives (Non Esterified …
1997
In human plasma, the cholesteryl ester transfer protein (CETP) plays a key role in lipoprotein metabolism by promoting the net mass transfer of cholesteryl esters from HDL towards apoB-containing lipoproteins, and the transfer of triglycerides from VLDL towards HDL and LDL. Thus CETP arises as a potentially important factor in plasma lipoproteins metabolism, a statement which raised a considerable interest in identifying the factors which may regulate CETP activity.In our in vitro studies, we demonstrated that amphipathic molecules (non esterified fatty acids and retinoic acids) constituted of one carboxylic head group and one hydrophobic carbon chain are able to increase the cholesteryl es…
Facile Synthesis of Fluorescent Polymer Nanoparticles by Covalent Modification-Nanoprecipitation of Amine-Reactive Ester Polymers
2015
Emission wavelength control in fluorescent nanoparticles (NPs) is crucial for their applications. In the case of inorganic quantum dots or dye-impregnated silica NPs, such a control is readily achieved by changing the size of the particles or choosing appropriate fluorescent dyes, respectively. A similar modular approach for controlling the emission wavelength of fluo-rescent polymer NPs, however, is difficult. This article reports on fluorescent polymer NPs, the synthesis of which provides a platform for a modular approach towards the preparation of fluorescent NPs of desired emission wavelength. Atom-transfer radical polymerization (ATRP) is employed to synthesize reactive ester polymers,…
Synthesis, computational evaluation and pharmacological assessment of acetylsalicylic esters as anti-inflammatory agents
2019
A convenient approach to the synthesis of alkyl esters of aspirin (ASA-OR) has been developed. The synthesis of ASA-OR has been realized in two steps: (1) direct esterification of salicylic acid with alcohols in the presence of dicyclohexylcarbodiimide to give alkyl salicylates (SAL-OR); (2) acetylation of SAL-OR with acetyl chloride to yield ASA-OR. Molecular mechanics simulations, performed to calculate the kinetic radii of several ASA-OR, indicated that the pentyl and hexyl acetylsalicylates possess the best properties to cross cell membranes. The in vitro biological tests demonstrate their anti-inflammatory activity, superimposable to that of aspirin. The results of our study suggest th…