845781-34-2Relevant articles and documents
Stereoselective synthesis of lower and upper rim functionalized tetra-α isomers of calix[4]pyrroles
Díaz-Moscoso, Alejandro,Hernández-Alonso, Daniel,Escobar, Luis,Arroyave, Frank A.,Ballester, Pablo
, p. 226 - 229 (2017)
Hydroxyaryl alkyl ketones with functionalized alkyl chains often fail to produce the corresponding tetra-α calix[4]pyrroles in Br?nsted acid mediated condensations with pyrrole. A remarkable effect exerted by the addition of methyltrialkylammonium chloride during the acid-mediated syntheses of a series of meso-(tetrahydroxyaryl)-meso-tetraalkylcalix[4]- pyrroles featuring alkyl terminal chloro or ester groups is reported. The ammonium salt enhances the cyclocondensation reaction and induces the almost exclusive formation of the tetra-α isomers.
A 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - ketone (by machine translation)
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Paragraph 0048; 0049; 0050, (2018/03/24)
The invention discloses a method for synthesizing 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - one method, its steps are: halogen anisole with glutaric anhydride reaction for the preparation of 5 - (3 - methoxyphenyl) - 5 - oxo-valeric acid, reducing 5 - (3 - methoxyphenyl) - 5 - oxo-valeric acid for the preparation of 5 - (3 - methoxyphenyl) pentanoic acid; 5 - (3 - methoxyphenyl) pentanoic acid through the intramolecular Friedel-crafts acylation reaction to obtain 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - one. The method of the invention the synthesis step is short, low cost, the total yield is high, can be used for industrial production. (by machine translation)
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.