POSITIVE ALLOSTERIC MODULATORS OF MUSCARINIC M2 RECEPTOR
申请人:Bayer Pharma Aktiengesellschaft
公开号:US20180297994A1
公开(公告)日:2018-10-18
The present application relates to positive allosteric modulators of the muscarinic M2 receptor, especially to novel 7-substituted 1-arylnaphthyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular disorders and/or renal disorders.
In this work, a simple and facile approach is conducted for preparing many new SBA-15 supported dendritic imidazolium ILs heterogeneous catalysts SBA-15/IL(1–3) having high ionic density from SBA-15. SBA-15/IL(3) as a green heterogeneous catalyst can be used for synthesis of 2-imidazolidinone from ethylenediamine and carbon dioxide and considering solvent-free condition. SBA-15/IL(3) showed to have
在这项工作中,采用一种简单易行的方法从 SBA-15 制备许多具有高离子密度的新型 SBA-15 负载的树枝状咪唑鎓 ILs 非均相催化剂 SBA-15/IL(1-3)。SBA-15/IL(3)作为一种绿色多相催化剂,可用于乙二胺和二氧化碳合成2-咪唑啉酮,并考虑无溶剂条件。SBA-15/IL(3) 表现出最高的催化活性,除了在 CO 2存在下对 2-咪唑啉酮的合成产率有积极的影响外,因为存在高密度外围两性离子离子液体官能团生物基 SBA-15/IL(3) 催化剂表面上的基团。 图形概要
Synthesis of 2-oxazolidones by sulfur-assisted thiocarboxylation with carbon monoxide and oxidative cyclization with molecular oxygen under mild conditions
作者:Takumi Mizuno、Junko Takahashi、Akiya Ogawa
DOI:10.1016/s0040-4020(02)00938-9
日期:2002.9
2-Aminoethanols were easily subjected to the thiocarboxylation with carbon monoxide promoted by elemental sulfur, followed by the oxidative cyclization with molecular oxygen to give corresponding 2-oxazolidones in good yields under mild conditions (1 atm, rt). Furthermore, 2-imidazolidones and 2-thiazolidone were also prepared in good yields similarly.
Ureaderivatives are obtained in mild to good yield from the reactions of primary aliphatic amines with CO2 in the absence of any catalysts, organic solvents or other additives. To optimize reaction conditions, experimental variables including temperature, pressure, the concentration of amine, reaction time etc. were studied. Satisfactory yields were obtained at the optimized conditions that are comparable