2-乙基唑来膦酸双核乙二胺铂配合物的合成与表征  

Synthesis and Characterization of 2-ethyl Zoledronic Acid Dinuclear Platinum-Ethylenediamine Complexes

作　　者：曹阳[1,2] 邱玲[1,2] 林建国[2] 罗世能[2] 夏咏梅 

机构地区：[1]江南大学化学与材料工程学院,江苏无锡214122 [2]江苏省原子医学研究所卫生部核医学重点实验室江苏省分子核医学重点实验室,江苏无锡214063

出　　处：《山东化工》2014年第5期7-11,共5页Shandong Chemical Industry

基　　金：江苏省医学重点人才基金(No.RC2011097);国家自然科学基金(No.21371082)

摘　　要：以2-乙基咪唑为原料在四丁基溴化铵为相转移催化剂的条件下与溴乙酸乙酯发生N-烷基化反应,再进行酯水解得到羧酸,之后与三氯化磷和磷酸发生磷酰化反应再进行水解得到2-(2-乙基-咪唑-1-基)-1-羟基乙烷-1,1-双膦酸(2-乙基唑来膦酸,EIDP)。以EIDP为配体,与硫酸根乙二胺铂在氢氧化钡存在的碱性条件下反应即得到目标产物2-乙基唑来膦酸双核乙二胺铂配合物{[Pt(en)]2EIDP},通过HPLC确认纯度,之后通过熔点、元素分析、红外光谱、质谱和1H-NMR对其结构进行了表征。分子结构为以双膦酸为配体的双核铂配合物,有望结合双膦酸的骨靶向性和铂基团的抗肿瘤活性。In the presence of tetrabutylammonium bromide （ TBAB ）, the reaction of 2 - ethyl imidazole with ethyl bromoacetate yielded corresponding ester. The product hydrolyzed to corresponding acetic acid. Phosphorus trichloride and phosphoric acid was added, respectively. After hydrolysis, EIDP was obtained. EIDP and Ba（ OH）2 was dissolved in water and [ Pt（en） （H20） （ OSO3 ） ] was added in the mixture with stirring. Finally, the filtrate was freeze - dried to afford white solid ultimate product {[ Pt （en）] 2EIDP}. The purity was confirmed by HPLC. The title complex was characterized by melting point, elemental analysis, IR, MS and ＇ H - NMR. This may lead to combination of bone affinity and antitumour activity.

关 键 词：2-乙基唑来膦酸 铂配合物 合成 结构表征 

分 类 号：TQ463[化学工程—制药化工]