2649-11-8Relevant articles and documents
Aliphatic thioethers by s-alkylation of thiols via trialkyl borates
Gunes, Deniz,Sirkecioglu, Okan,Bicak, Niyazi
experimental part, p. 1685 - 1690 (2010/09/17)
A simple and convenient one-pot procedure is described for the synthesis of thioethers via boron esters. This procedure involves in-situ generation of alkyl sulfates by reaction of trialkyl borates with concentrated sulfuric acid and subsequent reaction with thiols in the presence of pyridine. The reactions with boron esters of primary or secondary alcohols proceed cleanly at 100C and afford aliphatic thioethers in reasonable yields (59-93%) within 24 h. Interestingly, the 1H NMR spectra of the products showed no sign of positional isomerisms. The method fails however with thiophenol and does not yield aromatic thioethers, due to electrophilic substitution at the phenyl ring. Copyright Taylor & Francis Group, LLC.
Non-Polymeric Compositions for Controlled Drug Delivery
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, (2010/03/02)
The present invention provides a novel liquid composition suitable for in-situ formation of a depot system to deliver a bioactive substance in a controlled manner. The composition of the present invention comprises: (a) a hydrophobic non-polymeric carrier material; (b) a water miscible biocompatible organic solvent that dissolves the hydrophobic non-polymeric material; (c) an ionic complex that is formed between an amphiphilic molecule and a bioactive substance having a net charge at neutral pH in water. The present invention also provides a method of manufacturing and use of the composition thereof.
Synthesis and anti-influenza virus activity of 7-O-alkylated derivatives related to zanamivir
Honda, Takeshi,Masuda, Takeshi,Yoshida, Shuku,Arai, Masami,Kaneko, Satoru,Yamashita, Makoto
, p. 1925 - 1928 (2007/10/03)
A series of 7-alkyl ether derivatives related to zanamivir were synthesized using direct alkylation of the C-7 alcohol of sialic acid. Alkyl ether moiety of less than 12 carbons in length showed low nanomolar inhibitory activity against influenza A virus sialidase. Furthermore, their moiety improved influenza A virus plaque reduction activity compared to zanamivir. However, removal of the 8,9-diol of the 7-O-alkyl derivatives resulted in loss of antiviral potency. This result suggests that 8,9-diol must play an important role in binding with both influenza A and B virus sialidases.