[EN] ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITION THEREOF<br/>[FR] DÉRIVÉS AMINOESTÉRIFIÉS D'ALCALOÏDES ET COMPOSITION MÉDICINALE LES INCLUANT
申请人:CHIESI FARMA SPA
公开号:WO2010072338A1
公开(公告)日:2010-07-01
The present invention relates to alkaloid aminoester derivatives acting as muscarinic receptor antagonists, to methods of preparing such derivatives, to compositions comprising them and therapeutic use thereof.
Ugi four-component condensation with two cleavable components: the easiest synthesis of 2,N-diarylglycines
作者:Cristina Faggi、Ana G. Neo、Stefano Marcaccini、Gloria Menchi、Julia Revuelta
DOI:10.1016/j.tetlet.2008.01.134
日期:2008.3
The Ugi four-componentcondensation between anilines, aromatic aldehydes, isocyanides, and α-oxoacids afforded the expected adducts which were cleaved in mild conditions to give 2,N-diarylglycines in high yields.
ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITION THEREOF
申请人:Caligiuri Antonio
公开号:US20100173880A1
公开(公告)日:2010-07-08
Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
A possibility of obtaining fluorine-containing N-phenylphenylglycine derivatives at yields of up to 85% via the electrochemical carboxylation of corresponding benzalanilines was shown. The influence of imine's electron structure, the nature of supporting electrolyte and cathodic material on such processes is examined. It was found, that increasing electron accepting ability of the substituents in benzylidene and aniline fragments of the imine molecule lead to decrease of amino acid yields. The dependence of the N-phenyl-p-fluorophenylglycine yield on the cathode material (Zn, GC, Cu, Ag, Pt) and on the nature of the supporting electrolytes (Bu4NBr, Et4NBr, Et4NClO4, PhCH2Me3NClO4, LiBF4, LiClO4, NaBF4 and KBF4) Was investigated. The highest amino acid yields were obtained at cathodes (GC and Zn) that do not exhibit specific adsorption of fluorine-containing imines, as well as in the presence of background salts (Alk(4)NBr) whose cations do not show tendency to strong ion pairing with anion radicals formed by the electrochemical activation of the imines. (c) 2008 Elsevier B.V. All rights reserved.
Alkaloid aminoester derivatives and medicinal composition thereof