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

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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.