描述了一种高效的钯铜催化的炔丙基卤化物,芳基或杂芳基卤化物和仲胺的三组分组装。从易于获得的起始原料中,以高至优异的产率合成了多种叔炔丙基胺。当使用邻苯二甲酰亚胺钾或叔丁基亚氨基二碳酸酯代替仲胺时,这种三组分组装也是有效的。因此,它可以快速进入N-保护的炔丙基胺是合成伯和仲炔丙基胺的合适的中间体。以类似的方式,有效地获得了包括炔丙基酰胺,氨基甲酸酯和磺酰胺衍生物的相关化合物。该催化多米诺三组分工艺已成功地用于构建具有生物学意义的功能化2-(氨基甲基)苯并[ b ]呋喃或吲哚衍生物。
[EN] COMPOUNDS AND USE THEREOF FOR TREATMENT OF NEURODEGENERATIVE, DEGENERATIVE AND METABOLIC DISORDERS [FR] COMPOSÉS ET LEUR UTILISATION POUR LE TRAITEMENT DE TROUBLES NEURODÉGÉNÉRATIFS, DÉGÉNÉRATIFS ET MÉTABOLIQUES
Synthesis of Benzofurans and Indoles from Terminal Alkynes and Iodoaromatics Catalyzed by Recyclable Palladium Nanoparticles Immobilized on Siliceous Mesocellular Foam
作者:Alexandre Bruneau、Karl P. J. Gustafson、Ning Yuan、Cheuk-Wai Tai、Ingmar Persson、Xiaodong Zou、Jan-E. Bäckvall
DOI:10.1002/chem.201702614
日期:2017.9.18
(Pd0‐AmP‐MCF), for the synthesis of heterocycles. Reaction of o‐iodophenols and protected o‐iodoanilines with acetylenes in the presence of a Pd nanocatalyst produced 2‐substituted benzofurans and indoles, respectively. In general, the catalytic protocol afforded the desired products in good to excellent yields under mild reaction conditions without the addition of ligands. Moreover, the structure
The present invention provides compounds of the formula
which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.
Sulfonamide derivatives as glycokinase activators useful in the treatment of type 2 diabetes
申请人:Novartis AG
公开号:EP2298779A1
公开(公告)日:2011-03-23
The present invention provides compounds of the formula
which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (1) may be employed for the prevention and the-treatment of impaired glucose tolerance, type 2 diabetes and obesity,