CAS: 10128-06-0; α-Methyl-β-(3,4-Dimethoxyphenyl)-Alanin

上下游产品

3-(3,4-Dimethoxy-phenyl)-2-methyl-2-{[1-phenyl-meth-(E)-ylidene]-amino}-propionic acid methyl ester 4-bromomethyl-1,2-dimethoxybenzene

📜3,4-二甲氧基苄基溴置于苄基三乙基氯化铵 盐酸,氢氧化钾,Potassium Carbonate体系中,用 乙腈 用作溶剂,化学反应 30.0H,反应生成3-(3,4-二甲氧基苯基)-2-甲基丙氨酸
参考文献:苯甲醛亚胺的烷基化和亲核加成固相转移催化合成α-氨基酸
标题:苯甲醛亚胺的烷基化和亲核加成固相转移催化合成α-氨基酸
摘要:研究了在固-液相转移催化条件下,通过烷基化,迈克尔加成和羰基加成以及甘氨酸和丙氨酸酯衍生的亚胺与苯甲醛环加成,合成短而温和高效的α-氨基酸的路线.固液相转移催化反应的关键是为各种反应物选择碱.产量取决于所用的碱.讨论了使用koh,K 2 Co 3和na 2 Co 3获得的结果.研究了固液ptc苄基化反应的动力学,我们提出了一种可能的固液ptc机理作为界面自动催化程序.介绍了一些α-氨基酸合成的细节.
Doi:10.1016/s0040-4020(01)86041-5

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.