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

1. 2-脱氧-2-[^<18>F]氟-d -半乳糖的改进合成。用乙酰次萤石法合成了用于肝脏显像的新型放射性药物-2-脱氧-2-氟-d -半乳糖及其^<18> f标记化合物。使用2-脱氧-2-[^<18>F]氟d -半乳糖和PET研究肝功能。2-脱氧-2-氟-d -半乳糖的代谢物研究和临床Pet研究表明，该糖在肝功能研究中是一种非常有用的放射性药物。对这种糖的详细研究正在进行中。D-[1-^<11>C]己糖的合成[1]。D - [1 - ^ < 11 > C]葡萄糖。将d -阿拉伯糖和[^<11>C]氰化物的混合物在碱存在下加热10分钟，通过阳离子交换树脂柱，蒸发至干燥。用二硼烷处理残渣10分钟，得到所需的糖。D - [1 - ^ < 11 > C)半乳糖。用与(1)类似的方法处理D-葡萄糖和[1-^<11>C]氰化物的混合物，得到D-[1-^<11>C]半乳糖。2-脱氧-2-[^<18>F]氟乙酰胺-d -己糖的合成(1)。2-Deoxy-2 - [^ 18 > < F] fluoroacetamido-D-glucose。以[^<18>F]氟和溴乙酸乙酯为原料，实现了一锅高效合成糖的方法。该合成是通过卤素交换、碱性水解和缩合的结合来完成的。糖具有诊断性肿瘤显像活性。2-脱氧-2-[^<18>F]氟乙酰胺- d -甘露糖和- d -半乳糖。这两种糖的快速合成已经分别得到了发展，它们的生物学特性正在进一步研究中。

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.