2-(4’,4’-二膦酸基)丁酰氨基-3-(4-’N,N-二(β-氯乙基)氨基)苯基-丙酸的合成及初步的骨靶向性研究  

Synthesis of 2-(4',4'-diphosphono)Butyramido-3-(4'-(N,N-bi(β-chloroethyl))Amino)Phenyl-Propanoic Acid and its Bone Targeting Study

作　　者：陈沛[1] 张涛[1] 范琴[1] 曾建成[2] 吴勇[1] 

机构地区：[1]四川大学华西药学院药物化学研究室,成都610041 [2]四川大学华西医院,成都610041

出　　处：《四川大学学报（自然科学版）》2006年第3期706-709,共4页Journal of Sichuan University(Natural Science Edition)

基　　金：国家自然科学基金资助项目(39970869;30200286)

摘　　要：The immediate（3） was prepared via three steps: at first substitutionof diethyl phosphonite,as the initial material,followed by addition-elimination.After Michael Reaction withdiethylmalonate,hydrolyzation and decarboxylation,（3） converted into key immediate（6）,which was subsequentlyconjugated with Melphalan and specifically phosphonate cleaved.Then thetitle conjugate Awas achieved.Its structure was verified by（）1HNMR,IR,MS and it showed good bone targeting ability via hydroxyapatite adhesion testsin vitro.The immediate （3） was prepared via three steps： at first substitution of diethyl phosphonite, as the initial material, followed by addition-elimination . After Michael Reaction with diethyl m.lonate, hydrolyzation and decarboxylation , （3） converted into key immediate （6）, which was subsequently conjugated with Melphalan and specifically phosphonate cleaved. Then the title conjugate A was achieved. Its structure was verified by ^1HNMR, IR, MS and it showed good bone targeting ability via hydroxyapatite adhesion tests in vitro.

关 键 词：酰氨基 膦酸基 靶向性 氯乙基 合成 丙酸 苯基 多发性骨髓瘤 肿瘤治疗 治疗药物 

分 类 号：TQ637[化学工程—精细化工] TS194.45[轻工技术与工程—纺织化学与染整工程]