| 黄碧涌,赵洺良,姜永贺,等.以褐藻酸为载体的钆淋巴靶向MR造影剂的合成工艺研究[J].中国海洋药物,2019,38(5):31-36. |
| 以褐藻酸为载体的钆淋巴靶向MR造影剂的合成工艺研究 |
| Study on Synthetic Technology of Axillary Lymphatic Targeting Contrast Agent with Polymannuronic Acid as Carrier |
| 投稿时间：2019-04-30 修订日期：2019-05-05 |
| DOI： |
| 中文关键词: 甘露糖 工艺优化 DTPA |
| English Keywords:mannose DTPA process optimization |
| Fund Project: |
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| 中文摘要: |
| 淋巴核磁共振成像(MRI)作为一种分辨率高的非创伤性技术获得了广泛应用。本课题组以大分子褐藻酸为载体,连接1-O-氨基乙基甘露糖为其靶向基团,对氨基苄基二乙基三胺五乙酸螯合Gd 离子为磁共振造影影基团,形成钆淋巴靶向MR造影剂。本文旨在通过对1-O-氨基乙基甘露糖和对氨基苄基二乙基三胺五乙酸片段工艺路线优化以提升两者收率,进而提升终产物淋巴靶向造影剂的收率。其中1-O-氨基乙基甘露糖的合成中,变更合成方法,去除了危险剧毒易爆试剂叠氮钠的使用,反应步骤由六步减少到四步,且收率由3.6%提高到了37%,后处理简单易操作,适于放大制备；对氨基苄基二乙基三胺五乙酸片段的工艺优化主要为后处理方法的改进,易操作,且提高了收率,由原来的28%提升至57%。进一步以这两个片段为原料通过酰化、缩合及螯合反应成功制备造影剂,为后续的成药性研究提供了基础。 |
| English Summary: |
| Lymphoid magnetic resonance imaging (MRI) has been widely used as a high resolution non-invasive technique. Our group uses macromolecular alginic acid as carrier to link 1-O-aminoethylmannose as its targeting group, and p-aminobenzyldiethyltriamine pentaacetic acid chelate Gd ion as magnetic resonance imaging group. , forming a lymphatic-targeted MR contrast agent This paper aims to improve the yield of the end product lymphatic contrast agent by optimizing the route of 1-O-aminoethylmannose and p-aminobenzyldiethyltriamine pentaacetic acid.. In the synthesis of 1-O-aminoethylmannose, we changed the synthesis method, and the use of the |
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