175724-29-5Relevant articles and documents
Multi-arm single-molecular-weight polyethylene glycol and active derivative, preparation and application thereof
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Paragraph 0226; 0227; 0228; 0229; 0230, (2018/11/03)
The invention discloses multi-arm single-molecular-weight polyethylene glycol and an active derivative, preparation and application thereof. The multi-arm single-molecular-weight polyethylene glycol and the reactive derivative thereof are single molecular weight compounds, the application of a high molecular polymer mixture in the prior art is avoided, and the purity of a drug is effectively improved. When applied to drug modification, the multi-arm single-molecular-weight polyethylene glycol and the active derivative thereof can effectively improve the solubility, stability and immunogenicityof the drug, improve the absorption in vivo of the drug, prolong the half-life period of the drug, improve the bioavailability of the drug, enhance the efficacy of the drug, and reduce the toxic andside effects of the drug. Gel formed by the multi-arm single-molecular-weight polyethylene glycol active derivative provided by the invention can be used for preparing a slow release drug, prolongingthe action time of the drug, reducing the frequency of drug administrations, and improving patient compliance.
Synthesis of branched cores by poly-O-alkylation reaction under phase transfer conditions. A systematic study
Landeros, José M.,Silvestre, Hugo A.,Guadarrama, Patricia
, p. 412 - 419 (2013/04/23)
In the present paper is described a systematic study of poly-O-alkylation reactions of pentaerythritol (PE) and 1,1,1-tris(hydroxymethyl)ethane (TME) by 1,4 Michael addition, under phase transfer catalysis (PTC), considering the effect of: (1) the organophilicity of PTC (three different catalysts were tested), (2) PTC concentration (from catalytic to equimolar conditions), and (3) the regime of addition of reactants coexisting in the aqueous phase of the heterogeneous reaction system. The less organophilic transfer agent showed the best performance on these reactions. In our case, benzyltriethylammonium chloride (TEBAC) gathers the best features. The presence of NaOH as base, promotes the interfacial mechanism and not the bulk one. Out of the optimal range of concentration of NaOH (35-40%), competition between nucleophiles can occur, due to the saturation of the medium. Regarding the regime of addition of reactants, the scenario where NaOH and TEBAC are less time in contact, favors the formation of the desired products. Finally, the deprotection of tert-butyl groups of the poly-O-alkylated compounds is described, to get branched cores with terminal carboxylic acid groups in good yields (90-94%). Spectroscopic properties, such as IR, 1H and 13C NMR, of the synthesized compounds are also described.
New polypodal polycarboxylic ligands - Complexation of rare-earth ions in aqueous solution
Viguier, Romain,Serratrice, Guy,Dupraz, Agnes,Dupuy, Claude
, p. 1789 - 1795 (2007/10/03)
The complexation ability of new polypodal carboxylic ligands prepared from 2,2-bis(hydroxymethyl)-1-alkanols was investigated in aqueous solution with Y3+ and various lanthanide ions (La3+, Sm3+, Eu3+, Gd3+, Tb3+, Dy3+). The values of the stability constants for ML complexes are of the order of 104 for the hexadentate trioxypropionates, 107 for the hexadentate trioxyacetates and 1014 for the nonadentate triaminohexaacetates. In these systems, the nitrogens of the amino groups seem to be better chelating atoms than the oxygens of the ether groups. The hydration numbers of dysprosium(III) complexes have been determined from the DyIII-induced 17O NMR water shifts.
Polyalkylation of primary polyols by 1,4-addition to tert-butyl acrylate and acrylonitrile
Dupraz, Agnes,Guy, Philippe,Dupuy, Claude
, p. 1237 - 1240 (2007/10/03)
The very hydrophilic primary polyols pentaerythritol (PE), 1,1,1-tris(hydroxymethyl)ethane and tris(hydroxymethyl)aminomethane (TRIS), can be polyetherified in satisfactory yield by 1,4-addition to tert-butyl acrylate using phase-transfer catalysis. Polycyanoethylation of these polyols can also be accomplished with acrylonitrile. Preliminary results of chelation between some polyether-acids with samarium(III) are presented.