衣霉素类化合物的合成研究

发布时间：2018-07-12 16:27

本文选题：衣霉素 + 抗生素　；参考：《郑州大学》2017年硕士论文

【摘要】：衣霉素类化合物是直链脂肪酰胺类核苷抗生素,是一类微生物的特殊代谢产物,可以抑制生物体内GlcNAc-1-P转移酶的活性,进而抑制细菌细胞壁的形成。衣霉素具有很好的抗菌、抗病毒和抗癌活性。我们通过简单的原料尿嘧啶核苷在最开始引入衣霉素的碱基部分,再通过直链半乳糖烯醇硅醚片段与尿嘧啶核苷醛片段在SnCl4作为促进剂条件下发生Mukaiyama Aldol反应,能够以比较好的立体选择性得到偶联产物,然后经过氧化关环反应构建半乳糖环而成功得到了衣霉素类化合物关键母核结构Tunicaminyl uracil,后续以二糖结构为受体尝试与葡萄糖邻炔基苯甲酸酯片段在金催化剂作促进剂条件下发生糖苷化反应构建三糖片段。
[Abstract]:As a direct chain fatty amide nucleoside antibiotic, itramycin is a special metabolite of microorganism, which can inhibit the activity of GlcNAc-1-P transferase in organism, and then inhibit the formation of bacterial cell wall. Chlortetracycline has good antibacterial, anti-viral and anti-cancer activities. We introduced the base part of itamycin at the beginning through simple raw material uracil nucleoside, and then through the direct chain galactosylsilyl ether fragment and the uracil nucleoside aldehyde fragment under the condition of SNCL 4 as accelerator, the Mukaiyama Aldol reaction took place. The coupling products can be obtained with good stereoselectivity. Then the key parent nuclear structure of tunicaminyl uracilis was successfully obtained by the oxidation ring closing reaction. Then the dicosaccharide structure was used as the receptor to try to promote it with the glucose o alkynyl benzoate fragment in the gold catalyst. The glycoside reaction was carried out under the condition of the agent to construct the trisose fragment.
【学位授予单位】：郑州大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：TQ465

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