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摘要手性是自然界一种普遍现象，随着医疗技术的不断发展以及“反应停”等重大医药事故的发生，人们对单一手性对映体，特别是手性药物的单一异构体需求与日俱增，因此手性药物的拆分已经成为近几年来分析化学、药物化学领域非常有价值的研究课题之一。因为具有拆分效果好、分析速度快、进样量少、环境污染小等优点，符合绿色化学的宗旨，毛细管电泳技术(Capillary Electrophoresis，CE)已成为手性对映体分析、拆分方面的重要技术之一。同时手性选择剂的选择也是影响毛细管电泳技术分离手性药物效果的重要因素。目前，环糊精（Cyclodextrins）及其衍生物是毛细管电泳技术中应用最为广泛的手性选择剂。正电型环糊精与中性环糊精相比，又具有更好的水溶性，并且能够引入更强的氢键作用，从而能够在毛细管电泳以更低的浓度实现对多种消旋体药物更快速的手性拆分，对手性药物中也已体现出了相当优异的拆分能力。18981
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本论文制备了一种氢键作用增强正电型β-环糊精，单取代双正电中心型6A-双(2-甲氧基乙基)铵-β-环糊精氯盐（BMEtAMCD），在烷基铵类β-环糊精的基础上引入可以与消旋体产生氢键作用的甲氧基(-OCH3)，制备出新的正电型β-环糊精。
综上所述，本论文设计的新的双正电型环糊精衍生物6A-双(2-甲氧基乙基)铵-β-环糊精氯盐（BMEtAMCD）已被成功制备，所得产物经1HNMR 、13CNMR等表征。并利用毛细管电泳技术进行手性拆分实验，对酸性及两性消旋体实现了有效分离。研究结果为进一步了解环糊精提供了有效的科学依据。
关键词 正电型环糊精 氢键作用 毛细管电泳 手性拆分
毕业设计说明书（毕业论文）外文摘要
Title Design and application of bis-alkyl ammonium single substituted cationic β-cyclodextrins
Abstract
Chirality is a universal phenomenon in nature. With the continuous development of medical technology, people’s demands for single enantiomers of chiral drugs are increasing. Therefore, the separation of enantiomeric drugs has become an important issue in current society. Capillary electrophoresis（CE） has been one of the most important technologies in the field of chiral analysis due to its high separation efficiency, fast analysis speed and little sample consumption, less solvent pollution in consistent with the aim of green chemistry. To date, cyclodextrins（CDs）and their derivatives are the most widely used chiral selectors in CE. Compared with neutral CDs, cationic CDs can afford higher solubility in water and additional hydrogen bonding and electrostatic interactions can be included, good enantioseparations can thus be achieved with a lower concentration of cationic CD. These CDs have been exhibited an excellent chiral recognition ability in CE.
The present work mainly described one novel type of positively charged β-CDs, 6A-deoxy-bis(2-methoxyethyl)-ammonium- -β-CD chloride based on the introduction of an methoxyalkyl ammonium β-CD to form hydrogen bonding with the racemates, which produces a new type of positive-type β-CD.
In conclusion, the finely designed cationic CD, 6A-deoxyl-bis(2-methoxyethyl)- ammonium-β-cyclodextrin chloride（BMEtAMCD）has been synthesized. The obtained product was well confirmed by 1HNMR and 13CNMR characterization. Moreover, capillary electrophoresis technology was applied to racemic modification of anionic and ampholytic analytes. The work provides an effective scientific basis for the further study of cyclodextrins.
Keywords positively charged CD, hydrogen bonding, capillary electrophoresis chiral separation
目录
1. 绪论 1
1.1. 引言 1
1.2. 手性药物与药物手性的拆分技术 2