CAS: 23918-98-1; (2R,3R)-4-(6-Amino-9H-Purin-9-yl)-2,3-Dihydroxybutanoic Acid

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CAS号29789-09-1 5-(6-amino-puri... | CAS号35910-49-7 methyl 5-(6-ami... | CAS号25581-41-3 2,3-O-异亚丙基-D-赤酮酸内酯 | CAS号66224-66-6 6H-Purin-6-imin... | CAS号28875-69-6 2,3-O-cyclohexy...

📜D-Eritadenine Ethyl Ester置于sodium Hydroxide体系中,用95.5%的收率获得4-(9-腺嘌呤)-D-鞘氨醇-2,3-二羟基丁酸
参考文献:Synthesis And Antiviral Activity Of Stereoisomeric Eritadenines
标题:Synthesis And Antiviral Activity Of Stereoisomeric Eritadenines
摘要:D-厄利他呋喃核苷(ia)和l-厄利他呋喃核苷(iia)是从5-(腺嘌呤-9-基)-5-脱氧醛糖或对映异构的2,3-二取代的赤霉糖内酯(viiib,C,Xiv)制备而成.使用高碘酸盐在钌的存在下氧化甲基2,3-O-异丙基-D-核糖呋喃苷(ix),随后进行酸水解和硼氢化钠还原,得到l-核糖内酮(xi).将其2,3-O-异丙基衍生物经过碱水解,随后经过高碘酸盐氧化,硼氢化钠还原和与环己酮反应,得到2,3-O-环己基-L-赤霉糖内酯(xiv).[u-14C]-腺嘌呤与viiib缩合,经过酸水解,得到[u-14C-腺嘌呤]-D-厄利他呋喃核苷.通过高碘酸盐在钌的存在下氧化1-(腺嘌呤-9-基)-1-脱氧-2,3-O-异丙基脱氢醇(xvi)和(xvii),得到threo-厄利他呋喃核苷iii和iv.9-(2,2-二乙氧基乙基)腺嘌呤(xix)与丙二酸反应,得到4-(腺嘌呤-9-基)-3-丁烯酸(xxi);经过甲醇处理制备其甲酯(xxii),再与三乙胺异构化,得到甲基4-(腺嘌呤-9-基)-2-丁烯酸酯(xxiii).Xxiii的羟化反应得到d-和l-厄利他呋喃核苷的外消旋混合物(iii+iv).厄利他呋喃核苷ia和iia对牛痘病毒,麻疹病毒和水疱性口炎病毒具有活性.厄利他呋喃核苷ia也对副流感病毒和副流感病毒有效.总体而言,厄利他呋喃核苷的抗病毒活性按照d-赤霉糖(ia) > L-赤霉糖(iia) > D-和l-Threo(iii,Iv)的顺序递减.
Doi:10.1135/cccc19821392

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-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:KR-101513003-B1
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy compositions and applications

专利号:US-10814013-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:AU-2007308022-A2
优先权日:2006-10-05
标题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:AU-2007308022-A1
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications