CAS: 1874-54-0; Psicofuranine

📜N-Benzoyl-N,9-Bis(Trimethylsilyl)Adenin置于ammonium Hydroxide,Dowex 50 W X 8 (H+ Form),Tin(Ll) Chloride体系中,用 甲醇,水,乙腈 用作溶剂,化学反应 171.5H,反应生成阿洛酮糖腺苷
参考文献:脱氧硝基糖.第十七次沟通.由1-脱氧-1-Nitroribose酮糖衍生的核苷的合成†往最‡
标题:脱氧硝基糖.第十七次沟通.由1-脱氧-1-Nitroribose酮糖衍生的核苷的合成†往最‡
摘要:描述了从酮糖衍生的核苷的新方法.它基于1-脱氧-1-硝基醛糖的链延长,然后激活作为离去基团的硝基,并引入嘧啶或嘌呤碱.因此,通过醛醇缩合反应(4),3的端基异构硝基5/6的合成和6的臭氧分解由方案3制备了硝基醛糖7 (方案1).4的部分水解产生8/9,其表征为乙酸酯10/11,并转化为硝酮12/13.臭氧分解12/13得到14/15,将其乙酰化为16/17.7的亨利反应导致19和20,它们被乙酰化为21和22(方案2).将7的迈克尔迈克尔加成至丙烯腈和丙酸甲酯中,分别产生异构体23/24和25/26.简便的β消除可防止类似的16/17反应.因此,将硝基二醇15转化为原酸酯27,然后通过亨利反应,部分水解和乙酰化反应转化为28和29(方案2).通过x射线分析确定了19的结构.它是动力学控制的亨利反应7的主要产物.类似地,β-D-构型的硝基醛糖23和25是迈克尔加成的主要产物.这表明对衍生自7
Doi:10.1002/hlca.19910740719

专利信息

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:EP-0635577-B1
优先权日:1993-07-23
标 题 :Screen for inhibitors of melanin biosynthesis
发明人：BRINDLE FRANCES HARRIET ELIZAB; FROELIGER EUNICE HARRIET
权利人:BASF AG
摘要:A method for the identification of agents that inhibit melanin biosynthesis involves the incubation of test samples in cultures of a fungus that produces melanin. Observation of altered pigmentation in the culture or culture area containing test sample indicates inhibition of melanin biosynthesis. Preferred cultures for the screen contain a fungus that pigments in the light or the dark such as Cladosporium cucumerinum. Preferred embodiments employ test samples on disks or in wells in solidified cultures and a known melanin synthesis inhibitor as a positive control which is compared to the test sample by simple visual inspection.

专利号:CN-113462704-B
优先权日:2021-06-22
标题:Biosynthetic gene cluster of plant cytokinin angustmycin, biological material of biosynthetic gene cluster and application of biosynthetic gene cluster in synthesis of angustmycin

专利号:CN-113462704-A
优先权日:2021-06-22
标 题:A kind of biosynthetic gene cluster of plant cytokinin narrowomycin and its biological material and its application in the synthesis of narrowomycin