CAS: 630-60-4; Ouabain

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CAS号508-52-1 烏巴配基

(2R,3R,4R,5S,6S)-2-(((1R,3S,5S,8R,9S,10R,11R,13R,14S,17R)-11-Acetoxy-1,5,14-Trihydroxy-10-(Hydroxymethyl)-13-Methyl-17-(5-Oxo-2,5-Dihydrofuran-3-yl)Hexadecahydro-1H-Cyclopenta[a]Phenanthren-3-yl)Oxy)-6-Methyltetrahydro-2H-Pyran-3,4,5-Triyl Tribenzoate置于sodium Carbonate体系中,用 甲醇 作为反应溶剂,化学反应 1.0H,以88%的收率获得产物g毒毛旋花苷
参考文献:瓦巴加宁和哇巴因的全合成.
标题:瓦巴加宁和哇巴因的全合成.
摘要:
DOI:10.1002/anie.200704959

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-6362009-B1
优先权日:1997-11-21
标 题 :Solid phase synthesis of heterocycles
发明人：MUNOZ BENITO; CHEN CHIXU
权利人:MERCK & CO INC
摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-4761413-A
优先权日:1986-12-22
标 题:1,5-epoxy-2,3,4,5-tetrahydro-1H-3-benzazepins and use in treatment of ulcers
发明人：WACHTER MICHAEL P; KARANEWSKY DONALD S
权利人:ORTHO PHARMA CORP
摘要:The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.

专利号:US-4855426-A
优先权日:1986-12-22
标题:Process of preparing 1,5-epoxy-2,3,4,5-tetrahydro-1H-3-benzazepins
发明人：WACHTER MICHAEL P; KARANEWSKY DONALD S
权利人:ORTHO PHARMA CORP
摘要:The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.

专利号:US-5519131-A
优先权日:1991-04-15
标题:Synthesis of pyridooxazinyl-indoles
发明人：EFFLAND RICHARD C; DAVIS LARRY; OLSEN GORDON E
权利人:HOECHST MARION ROUSSEL INC
摘要:This application relates to a process for the preparation of indolylpyridooxazines of the formula wherein R1, R2 and R3 are as defined in the specification which comprises cyclizing compound of the formula in the presence of a strong base such as sodium hydride or potassium t-butoxide.