Synthesis and cholinesterase activity of phenylcarbamates related to Rivastigmine, a therapeutic agent for Alzheimer's disease
摘要:
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. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
[EN] 2-OXO-3,4-DIHYDROPYRIDINE-5-CARBOXYLATES AND THEIR USE<br/>[FR] 2-OXO -3,4-DIHYDROPYRIDINE -5-CARBOXYLATES ET LEUR UTILISATION
申请人:UNIV LILLE II DROIT & SANTE
公开号:WO2016016238A1
公开(公告)日:2016-02-04
The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.
本发明涉及公式(I)的新化合物,其药用盐或溶剂和它们的用途。
Metal-free regioselective hydrochlorination of unactivated alkenes<i>via</i>a combined acid catalytic system
作者:Shengzong Liang、Gerald B. Hammond、Bo Xu
DOI:10.1039/c7gc03665e
日期:——
A combined acid HCl/DMPU-acetic acid catalytic system was used in the hydrochlorination of a wide range of unactivated alkenes.
一个结合了盐酸/HCl、DMPU和乙酸的催化体系被用于对一系列未活化的烯烃进行氯化反应。
Enantioselective Electroreductive Coupling of Alkenyl and Benzyl Halides via Nickel Catalysis
作者:Travis J. DeLano、Sarah E. Reisman
DOI:10.1021/acscatal.9b01785
日期:2019.8.2
An electrochemically-driven enantioselective nickel-catalyzed reductive cross-coupling of alkenyl bromides and benzylchlorides is reported. The reaction forms products bearing allylic stereogenic centers with good enantioselectivity under mild conditions in an undivided cell. Electrochemical activation and turnover of the catalyst mitigate issues posed by metal powder reductants. This report demonstrates