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Chemical Synthesis of Biologically Active Substances Labeled with Positron Emitting Radionuclides for Diagnoses of Deceases of Brain and Heart, and Cancer

化学合成正电子发射放射性核素标记的生物活性物质，用于诊断脑部和心脏疾病以及癌症

基本信息

批准号：
62480236
负责人：
TADA Masao
金额：
$ 4.29万
依托单位：
Tohoku University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (B)
财政年份：
1987
资助国家：
日本
起止时间：
1987 至 1989
项目状态：
已结题

项目摘要

1. Improved synthesis of 2-deoxy-2-[^<18>F]fluoro-D-galactose.Chemical synthesis of 2-deoxy-2-fluoro-D-galactose and its ^<18>F-labeled compound, a new radiopharmaceutical for liver imaging, using the acetyl hypofluorite procedure has been achieved.2. Liver function studies using 2-deoxy-2-[^<18>F]fluoro-D-galactose and PET.Both metabolite study and clinical Pet study on 2-deoxy-2-[^<18>F]fluoro-D-galactose show that the sugar is a very useful radiopharmceutical for the liver function studies. The detailed study on the sugar is in progress.3. Synthesis of D-[1-^<11>C]hexoses.(1). D-[1-^<11>C]Glucose. A mixture of D-arabinose and [^<11>C]cyanide was heated for 10 min in presence of alkali, passed through a column of cation exchange resine, and evaporated to dryness. The residue was treated with the diborane for 10 min to afford the desired sugar.(2). D-[1-^<11>C]Galactose. A mixture of D-lyxose and [^<11>C]cyanide was treated in a similar manner as in (1) to give D-[1-^<11>C]galactose.4. Synthesis of 2-deoxy-2-[^<18>F]fluoroacetamido-D-hexoses.(1). 2-Deoxy-2-[^<18>F]fluoroacetamido-D-glucose. An efficient, one-pot synthesis the sugar starting from [^<18>F]fluoride and ethyl bromoacetate has been achieved. The synthesis is accomplished by a combination of halogen exchange, alkaline hydrolysis, and condensation. The sugar showed the diagnostic tumor-imaging activity.(2). 2-Deoxy-2-[^<18>F]fluoroacetamido-D-mannose and -D-galactose. Rapid synthesis of theses sugars, respectively, have been developed,and their biological characteristics are being further investigated.

1. 2-脱氧-2-<18>氟-D-半乳糖的合成方法改进：采用乙酰基次氟酸盐法化学合成了2-脱氧-2-氟-D-半乳糖及其<18>标记物（一种新的肝显像药物）.用2-脱氧-2-[~（13 <18>F）]氟-D-半乳糖和PET研究肝功能2-脱氧-2-[~（13 F）]氟-D-半乳糖的代谢物研究和临床PET研究表明，2-脱氧-2-[~（13 <18>F）]氟-D-半乳糖是一种非常有用的肝功能研究放射性药物。对糖的详细研究正在进行中。D-[1- 1C<11>]己糖的合成。（一）. D-[1-^<11>C]葡萄糖。将D-阿拉伯糖和[2C<11>]氰化物的混合物在碱的存在下加热10分钟，使其通过阳离子交换树脂柱，并蒸发至干。将残余物用乙硼烷处理10分钟，得到所需的糖。（二）、D-[1-^<11>C]半乳糖。D-来苏糖和[13 <11>C]氰化物的混合物以与（1）中类似的方式处理，得到D-[1- 13 <11>C]半乳糖。合成2-脱氧-2-[13 <18>F]氟乙酰胺基-D-己糖。（一）. 2-脱氧-2-[13 <18>F]氟乙酰氨基-D-葡萄糖。以氟代<18>物和溴乙酸乙酯为原料，实现了一锅法高效合成糖。该合成通过卤素交换、碱性水解和缩合的组合来完成。糖显示出诊断肿瘤成像活性。（二）、2-脱氧-2-[13 <18>F]氟乙酰氨基-D-甘露糖和-D-半乳糖。这些糖的快速合成方法已经开发出来，它们的生物学特性正在进一步研究中。