CAS: 2101-86-2; 1-Azido-4-Methylbenzene

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📜4-甲基苯胺盐酸盐置于sodium Nitrite体系中,化学反应生成P-叠氮甲苯
参考文献:新型1,2,3-三唑基连接苯并咪唑酮的高效简单合成,分子对接及抗菌活性评价
标题:新型1,2,3-三唑基连接苯并咪唑酮的高效简单合成,分子对接及抗菌活性评价
摘要:摘要 在这项研究中,通过叠氮化物与苯并咪唑酮 2A-B 的点击反应合成了一系列新型 1,2,3-三唑基-苯并咪唑酮衍生物.后一种化合物以优异的收率(85-97%)制备,产物的结构通过光谱分析确定.然后,化合物 7A 的 X 射线晶体分析揭示了自组装特性.评估了新的杂环化合物对革兰氏阳性菌和革兰氏阴性菌以及真菌菌株的体外抗菌活性.测试最多的合成化合物对所有测试菌株均显示出有效的抗菌和抗真菌活性.发现化合物 6C 是最有活性的,特别是对黑曲霉和青霉菌的活性.具有相同的 Mic 和 Mbc 为 0.0625 Mg/ml.此外,计算机分子对接研究表明,实验活性与计算的结合亲和力之间存在非常好的相关性.根据对接结果,化合物6D显示出最小的结合能,可以认为是一种非常好的抗菌剂.图形概要
Doi:10.1080/00397911.2020.1803913

专利信息

专利号:US-2004058888-A1
优先权日:2000-01-13
标题:Methods for synthesis of alpha-d-gal (1~>3) gal-containing oligosaccharides
发明人：BORNAGHI LAURENT; DEKANY GYULA; DRINNAN NICHOLAS BARRY; PAPAGEORGIOU JOHN; WEST MICHAEL LEO
摘要:This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R 3 is methoxy or methyl; R 1 is H, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R 2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4 -chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.

专利号:US-2005014954-A1
优先权日:2001-11-22
标 题:Pyrrole synthesis
发明人：OHRLEIN REINHOLD; BAISCH GABRIELE
摘要:The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.

专利号:US-8026383-B2
优先权日:2001-07-06
标题:Process for the preparation of intermediates useful in the synthesis of statin derivatives
发明人：OEHRLEIN REINHOLD; BAISCH GABRIELE; END NICOLE; BURKHARDT STEPHAN; STUDER MARTIN
权利人:BASF SE
摘要:The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I n nwherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH 3 )OCH 3 , R a is a hydroxy-protecting group and R b is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.

专利号:US-7569686-B1
优先权日:2006-01-27
标题:Compounds and methods for synthesis of bicyclic nucleic acid analogs
发明人：BHAT BALKRISHEN; XIA JIE; SETH PUNIT P; VASQUEZ GUILLERMO; MIGAWA MICHAEL T; ALLERSON CHARLES; PRAKASH THAZHA P; SWAYZE ERIC E
权利人:ISIS PHARMACEUTICALS INC
摘要:The present invention provides compounds and methods of using them for preparing bicyclic nucleosides. The bicyclic nucleosides are useful for preparing chemically modified oligomeric compounds. Oligomeric compounds comprising these bicyclic nucleosides have enhanced properties such as increased nuclease resistance.

专利号:US-8487094-B2
优先权日:2008-07-25
标题 :Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
发明人：FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA
权利人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA; BOEHRINGER INGELHEIM INT
摘要:Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).

专利号:US-2012095211-A1
优先权日:2010-09-22
标 题 :Substituted proline inhibitors of hepatitis c virus replication
发明人：BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D
权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC
摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.