7035-04-3Relevant articles and documents
Benzofuran-derived benzylpyridinium bromides as potent acetylcholinesterase inhibitors
Baharloo, Farzaneh,Moslemin, Mohammad Hossein,Nadri, Hamid,Asadipour, Ali,Mahdavi, Mohammad,Emami, Saeed,Firoozpour, Loghman,Mohebat, Razieh,Shafiee, Abbas,Foroumadi, Alireza
, p. 196 - 201 (2015/03/05)
A series of benzofuran-based N-benzylpyridinium derivatives 5a-o were designed and synthesized as novel AChE inhibitors. The synthetic pathway of the compounds involved the preparation of 4-(benzofuran-2-yl)pyridine intermediates via the reaction of different salicylaldehyde derivatives and 4-(bromomethyl)pyridine, followed by intramolecular cyclization. Subsequently, the 4-(benzofuran-2-yl)pyridines were N-benzylated by using appropriate benzyl bromide to afford the final product 5a-o. The results of in vitro AChE activity evaluation of synthesized compounds revealed that all compound had potent anti-AChE activity comparable or more potent than standard drug donepezil. The N-(3,5-dimethylbenzyl) derivative 5e with IC50 value of 4.1 nM was the most active compound, being 7-fold more potent than donepezil.
One-pot synthesis of useful heterocycles in medicinal chemistry using a cascade strategy
Wu, Guiyong,Yin, Weiyu,Shen, Hong C.,Huang, Yong
supporting information; experimental part, p. 580 - 585 (2012/04/23)
To access useful heterocycles in medicinal chemistry such as pyridazinones, dihydropyrimidinones, and dihydropyrimidinthiones, a "green" mild and highly efficient one-pot triple cascade was developed involving a Claisen-decarboxylation, electrophilic reaction, and subsequent heterocyclization. In addition, indazoles and benzofurans could also be constructed via a double cascade. To develop the cascade process, a direct Claisen-decarboxylation reaction was firstly optimized. This reaction can then couple with electrophilic reactions including alkylation, Michael addition or aldol reaction to enable the preparation of various aryl ketones in a one-pot fashion. The Royal Society of Chemistry 2012.