CAS: 54867-56-0; Bufrolin

📜6-Butyl-4,10-Dioxo-1,4,7,10-Tetrahydro-[1,7]Phenanthroline-2,8-Dicarboxylic Acid Dimethyl Ester置于sodium Hydroxide体系中,用 碳酸氢钠 作为反应溶剂,化学反应生成 丁夫罗林
参考文献:Pharmaceutical Compositions Comprising Pyridoquinoline Derivatives And
标题:Pharmaceutical Compositions Comprising Pyridoquinoline Derivatives And
摘要:含有2,7-二羧基-4,9-二羟基吡啶并[2,3-G]喹啉衍生物或2,8-二羧基-4,6-二羟基吡啶并[3,2-G]喹啉衍生物的药物组合物.这些化合物对由抗原-抗体反应引发的综合症或疾病具有活性.还公开了制备这些化合物的方法.

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.