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Design and Synthesis of Novel Polyester-type Dendrimers Having Cell Recognition Ability.

具有细胞识别能力的新型聚酯型树枝状聚合物的设计与合成。

基本信息

批准号：
13680677
负责人：
IWAMURA Michiko
金额：
$ 2.24万
依托单位：
Toho University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2001
资助国家：
日本
起止时间：
2001 至 2003
项目状态：
已结题

项目摘要

The purpose of this research project is design and synthesis of a new polyester-type dendritic skeleton that is biodegradable and applicable to a dendritic caged compound, a new drag delivery system.The building block was synthesized using acetoacetic acid ester synthesis of benzyl acetoacetate and t-butyl acrylate. 2:1 addition product was obtained > 90% after addition, hydrogenolysis and decarboxylation. The optimum reaction conditions for dendrimer synthesis were examined. The dendrimers from [G1, MW: 821] to [G5, MW: 15327] were obtained in an average more than 80% yield by divergent method using iterative reaction using [deprotection by HCOOH then condensation by EDCI/DMAP]. They were easily purified by silica gel column chromatography using hexane and ethyl acetate (1:1 v/v). The dendrimers thus obtained were colorless viscous liquid that was soluble in organic solvents such as dichloromethane or ethyl acetate. The structural characterization was carried out by elemental analysis, NMR, and ESI-MS. ^1H and ^<13>C NMR signals were accurately assigned using versatile NMR measurement techniques such as NOESY, ROESY, HMBC. Also, the conformational mobility of outer and inner shells of these dendrimers were assessed by ^<13>C NMR relaxation time (T_1).For the application of these dendrimers, tetraethylen glycol, 1-pirenyl, or sugar derivatives were indroduced at their peripbhery. Their characterization was now in progress.

本研究的目的是设计合成一种可生物降解的新型聚酯型树枝状骨架，并将其应用于树枝状笼状化合物的新型阻力输送系统中。经加成、氢解、脱羧基后，得到2：1加成产物&gt；90%。考察了合成树枝状大分子的最佳反应条件。用发散法合成了从[G1，Mw：821]到[G5，Mw：15327]的树枝状大分子。用正己烷和乙酸乙酯(1：1v/v)作硅胶柱层析，纯化效果好。得到的树枝状大分子为无色粘性液体，可溶于二氯甲烷或乙酸乙酯等有机溶剂。通过元素分析、核磁共振、电喷雾质谱等手段对其结构进行了表征。使用多种核磁共振测量技术(如NOESY、ROESY、HMBC)准确地指定了^1H和^&lt；13&gt；C核磁共振信号。此外，还用核磁共振弛豫时间(T_1)测定了这些树枝状大分子的外壳层和内层的构象迁移率。为了应用这些树状大分子，在其周围引入了四乙烯二醇、1-螺环烯或糖的衍生物。他们的角色现在正在进行中。