92912-56-6Relevant articles and documents
Synthesis and cholinesterase activity of phenylcarbamates related to Rivastigmine, a therapeutic agent for Alzheimer's disease
Mustazza, Carlo,Borioni, Anna,Giudice, Maria Rosaria Del,Gatta, Franco,Ferretti, Rosella,Meneguz, Annarita,Volpe, Maria Teresa,Lorenzini, Paola
, p. 91 - 109 (2007/10/03)
In order to develop new cholinesterase agents effective against Alzheimer's disease (AD) we synthesized some phenylcarbamates structurally related to Rivastigmine and evaluated their in vitro and in vivo biological activity. Among the compounds which displayed the most significant in vitro activity, 1-[1-(3-dimethylcarbamoyloxyphenyl)ethyl]piperidine (31b), in addition to a simple and cheaper synthesis, showed lower toxicity and very similar therapeutic index in comparison with Rivastigmine.
A facile one-carbon homologation of aryl aldehydes to amides.
Shen, Wang,Kunzer, Aaron
, p. 1315 - 1317 (2007/10/03)
The easily accessible 2-aryl-1,1-dibromo-1-alkenes can be converted to amides under unusually mild conditions in good to excellent yields. Both electron-donating and electron-withdrawing substitutions on the aromatic rings are tolerated, and the reaction works well with hindered alkylamines. This simple homologation could find broad applications. [reaction: see text]
Electro-organic Reactions. Part 22. An Entry into the Quinolizidine and Benzoquinolizidine Ring Systems via Anodic Methoxylation
Palasz, Peter D.,Utley, James H. P.,Hardstone, J. David
, p. 281 - 292 (2007/10/02)
Examples of the quinolizidine and benzoquinolizidine ring systems (1,1-bisethoxycarbonyl-4-oxo-quinolizidine, 1,3,4,6,7,11b-hexahydro-2H-benzoquinolizidine, and 1,2-t-butyl-3,4,6,7,11b-hexahydro-2H-benzo-quinolizidine) have been synthesized by routes which involve initial anodic methoxylation of piperidine precursors with subsequent intramolecular Lewis acid-catalysed cyclisation reactions.Reaction conditions for such cyclisations have been explored; success depends on a correct choice of catalyst (usually aluminium chloride) and, critically, on steric factors.The stereochemistry of the cyclic products has been established and the stereochemical course of the reactions is commented upon.