聚乙二醇及其衍生物的合成研究
發(fā)布時(shí)間:2018-03-22 06:00
本文選題:聚乙二醇 切入點(diǎn):十二甘醇 出處:《華東師范大學(xué)》2017年碩士論文 論文類(lèi)型:學(xué)位論文
【摘要】:聚乙二醇是一類(lèi)由乙二醇聚合而成的化合物。聚乙二醇具有無(wú)毒、無(wú)免疫原性、無(wú)抗原性、生物相容性良好、價(jià)廉易得等優(yōu)點(diǎn),能夠與各種藥物通過(guò)共價(jià)鍵或者非共價(jià)鍵的方式偶聯(lián),PEG修飾的藥物能大大增加藥物水溶性并增加在體內(nèi)的穩(wěn)定性,并延長(zhǎng)藥物半衰期。目前聚乙二醇合成方法報(bào)道較少,本文旨在探究新型的單分散聚乙二醇及聚乙二醇衍生物的合成方法,并設(shè)計(jì)以聚乙二醇為親水端的新型材料。論文第一部分工作研究了單分散聚乙二醇的合成方法,對(duì)傳統(tǒng)的單分散聚乙二醇合成工藝進(jìn)行了改進(jìn),且該改進(jìn)路線具有一定的普適性。此外還對(duì)單分散聚乙二醇氨基化衍生物的合成做了探究,發(fā)展了一條路線短、操作簡(jiǎn)單合成工藝,降低了單分散聚乙二醇氨基化衍生物的生產(chǎn)成本。最后我們還對(duì)mPEG-NH2的合成方法進(jìn)行了優(yōu)化,設(shè)計(jì)出了一種基于Mitsunobu反應(yīng)的新型mPEG-NH2合成方法,該方法相較于傳統(tǒng)方法操作大大簡(jiǎn)便,且產(chǎn)品質(zhì)量得到了顯著提升。論文的第二部分中,我們?cè)O(shè)計(jì)出兩個(gè)聚乙二醇修飾的自裂解材料,均以mPEG-NH2為親水端,以多個(gè)碳酸酯與氨基甲酸酯為骨架,并分別以硼酸酯與硝基為觸發(fā)點(diǎn)。首先我們研究了化合物親脂端的具體合成方法,在完成化合物的合成之后探究了兩個(gè)化合物在水中自組裝的情況,此外我們希望探究其在過(guò)氧化氫環(huán)境下與還原環(huán)境下的穩(wěn)定性。
[Abstract]:Polyethylene glycol (PEG) is a class of compounds polymerized from ethylene glycol. Polyethylene glycol has the advantages of non-toxic, non-immunogenicity, no antigenicity, good biocompatibility, cheap and easy to obtain, etc. Drugs that can be coupled with various drugs by covalent or non-covalent bonds can greatly increase their water solubility, increase their stability in vivo and prolong their half-life. The purpose of this paper is to study the synthesis method of monodisperse polyethylene glycol and its derivatives, and to design a new kind of material with polyethylene glycol as hydrophilic end. The first part of this paper studies the synthesis method of monodisperse polyethylene glycol. The traditional synthesis process of monodisperse polyethylene glycol is improved, and the improved route has certain universality. In addition, the synthesis of monodisperse polyethylene glycol amino derivatives has been explored, and a short route has been developed. The production cost of monodisperse poly (ethylene glycol) amino derivatives was reduced. Finally, the synthesis method of mPEG-NH2 was optimized, and a new mPEG-NH2 synthesis method based on Mitsunobu reaction was designed. Compared with the traditional method, the method is much easier to operate, and the quality of the product has been greatly improved. In the second part of the thesis, we designed two polyethylene glycol modified self-pyrolysis materials with mPEG-NH2 as hydrophilic terminal. Several carbonates and carbamate were used as the skeleton, and borate and nitro were used as trigger points respectively. Firstly, we studied the specific synthesis method of lipophilic end of compounds. After the synthesis of the compounds, the self-assembly of the two compounds in water was investigated. In addition, we hope to investigate the stability of the compounds in hydrogen peroxide and reduction environment.
【學(xué)位授予單位】:華東師范大學(xué)
【學(xué)位級(jí)別】:碩士
【學(xué)位授予年份】:2017
【分類(lèi)號(hào)】:O632.3
【參考文獻(xiàn)】
相關(guān)期刊論文 前1條
1 熊成東,王亞輝,袁明龍,鄧先模;聚乙二醇衍生物的合成研究進(jìn)展[J];高分子通報(bào);2000年01期
,本文編號(hào):1647345
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