Search results for "synthesis"
showing 10 items of 2844 documents
Electrosynthesis as a powerful method for the generation of catalytic intermediates: efficient isolation of a palladium aryl halide oxidative additio…
2011
International audience; Polyphosphane ligands of controlled conformation promote highly efficient palladium-catalyzed cross-coupling reactions. Electrosynthesis has been used as a new straightforward method to obtain important intermediates in the search for a better mechanistic understanding. As a proof of concept, the facile synthesis of a phenyl iodopalladium(II) complex (2) was conducted at the electrolysis scale from a readily electrogenerated unstable Pd0 precursor.
Experimental and theoretical investigations for the regio and stereoselective transformation of trans 1,2,3-trisubstituted aziridines into trans oxaz…
2003
The regio and stereoselective transformation of trans 1,2,3-trisubstituted aziridines into trans oxazolidin-2-ones takes place in good yield. However, the cis configuration at C2 and C3 in monocyclic aziridines is a limiting factor for this transformation. Ab initio calculations show that while the ring-opening process assisted by iodide is regioselective, the subsequent ring-closure is responsible for the retention of the configuration at the trans oxazolidin-2-ones. The larger energy found for the ring-closure process for the cis aziridines accounts for the non-formation of the cis oxazolidin-2-ones.
Pig liver esterase (PLE)-mediated resolution of N-substituted 4-benzoyloxy-3-carbomethoxypiperidines: A convenient preparation of 4-hydroxy- and 4-be…
2000
Abstract Pig liver esterase (PLE) afforded smooth chemical resolution of racemic N -substituted 4-(benzoyloxy)-3-carbomethoxypiperidines. The enzyme showed good chemo- and enantioselective properties, thus allowing discrimination between the carbomethoxy and benzoate ester groups, the latter being more easily hydrolyzed. The proposed methodology also represents a practical means for the procurement of N -substituted 4-hydroxy-3-carbomethoxypiperidines in enantiomerically pure form.
Prebiotic polypeptides and the origin of biological information.
1983
Recent data on the origin of biological information are reviewed. These data corroborate the view that polyamino acids were the first informational polymers. The source of information is seen in the chemical reactivity of amino acids, their prebiotic abundance and the prebiotic environment. Evidence is presented in favor of Matsuno's protohypercycle that may have preceded Eigen's hypercycle, but that involves a translation of information from polypeptides into that of polynucleotides.
Effect of Glufosinate (Phosphinothricin) and Inhibitors of Photorespiration on Photosynthesis and Ribulose-1,5-Bisphosphate Carboxylase Activity
1992
Summary Glufosinate (phosphinothricin) irreversibly inhibits glutamine synthetase and leads to a great decrease in the amino acids glutamine, glutamate, aspartate, serine, glycine and alanine. Due to the lack of glutamate and serine, the transamination of glyoxylate into glycine in the course of photorespiration cannot take place. The inhibition of this part of the photorespiratory process plays the essential role with respect to the photosynthesis inhibition caused by PPT under atmospheric conditions. After addition of different photorespiration or Calvin cycle intermediates to phosphinothricin no decrease in photosynthesis inhibition can be measured. This suggests that photosynthesis inhi…
Design, synthesis, biological evaluation and molecular modelling of substituted pyrrolo[2,1-a]isoquinolinone derivatives: discovery of potent inhibit…
2021
We report here the design, synthesis and biological evaluation of a new series of substituted pyrrolo[2,1-a]isoquinolin-3-one derivatives, some of which have strong inhibitory activity against both AChE and BChE enzymes. The design of these new inhibitors was carried out taking rivastigmine as the starting structure. Thus, on the basis of an exhausting molecular modeling study using combined techniques (docking, dynamic molecular simulations and QTAIM calculations), we obtained new ligands possessing stronger inhibitory effects than rivastigmine, the reference compound. QTAIM analysis gave us detailed information about the molecular interactions stabilizing the different ligand–enzyme compl…
Chemical Synthesis of 2′-O-Alkylated siRNAs
2010
Chemical synthesis has been a major endeavor to create active siRNAs. The downregulation of mRNA by 21-mer double-stranded siRNAs can be improved by using modified nucleotides, especially 2'-O-alkylated ones. Besides the commercially available 2 cent-O-methyl ribosides, 2'-alkyl groups bearing positive charges are especially promising candidates. We have shown that in a proper formulation they are superior to unmodified siRNAs. This may be due to enhanced stability and most probably to a better uptake into the cells.