📜4-溴苯腈置于溴,碘,Magnesium体系中,用 乙醚 用作溶剂,化学反应 6.0H,反应生成2,4'-二溴苯丙酮 参考文献:Substituted 2-Aminothiazoles Are Exceptional Inhibitors Of Neuronal Degeneration In Tau-Driven Models Of Alzheimer's Disease 标题:Substituted 2-Aminothiazoles Are Exceptional Inhibitors Of Neuronal Degeneration In Tau-Driven Models Of Alzheimer's Disease 摘要:A Novel Series Of 2-Aminothiazoles With Strong Protection In An Alzheimer'S Disease (Ad) Model Comprising Tau-Induced Neuronal Toxicity Is Disclosed. These Derivatives Can Be Synthesized In One-Pot And A Small Sar Of The Substitution Within These Series Afforded Several Compounds That Counteracted Tau-Induced Cell Toxicity At Nanomolar Concentrations. These Congeners Therefore Have Strong Potential As Possible Treatment For Alzheimer'S Disease And Other Related Tauopathies. (C) 2011 Elsevier B.V. All Rights Reserved. Doi:10.1016/j.Ejps.2011.05.014
专利号:US-7977371-B2 优先权日:2007-02-26 标题 :Pyrrole derivative having ureido group and aminocarbonyl group as substituents 发明人:KAWASHIMA KENJI; ENOMOTO HIROSHI; ISHIZAKA NORIKO; YAMAMOTO MINORU; KUDOU KAZUHIRO; MURAI MASAAKI; INABA TAKAAKI; OKAMOTO KAZUYOSHI 权利人:SANTEN PHARMACEUTICAL CO LTD 摘要:Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; R 1 represents a halogen atom, a hydrogen atom, a lower alkyl group or the like; R 2 represents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group, a lower alkynyl group which may have a substituent, a lower cycloalkyl group, an aryl group, a hydroxy group, a lower alkoxy group which may have a substituent or the like; and n represents 0, 1, 2, 3 or the like.
摘要:Collings, J. C., Science of Synthesis Knowledge Updates, (2013) 4, 235. 摘要:Vilhelmsen, M. H., Science of Synthesis Knowledge Updates, (2014) 2, 363. 摘要:Stoltz, B. M.; Mohr, J. T., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 669. 摘要:Stoltz, B. M.; Mohr, J. T., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 662. 摘要:Shimizu, M.; Hiyama, T., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 575.