1989 Fiscal Year Final Research Report Summary
Chemical Synthesis of Biologically Active Substances Labeled with Positron Emitting Radionuclides for Diagnoses of Deceases of Brain and Heart, and Cancer
| Project/Area Number |
62480236
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| Research Category |
Grant-in-Aid for General Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Radiation science
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| Research Institution | Tohoku University |
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Principal Investigator |
TADA Masao Tohoku Univ., Res.Inst. for TB and Cancer, Assoc.Prof., 抗酸菌病研究所, 助教授 (10006083)
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| Co-Investigator(Kenkyū-buntansha) |
KUBOTA Kazuo Tohoku Univ., Res.Inst. for TB and Cancer, Instr., 抗酸菌病研究所, 講師 (40161674)
ITO Masatoshi Tohoku Univ., Cyclotron and RI Center, Assoc.Prof., サイクロトロンラジオアイソトープセンター, 助教授 (00125501)
SUGIYAMA Hiroshi Tohoku Univ., Chem.Res.Inst. of Non-aq.Solu., Assoc.Prof., 非水溶液化学研究所, 助教授 (90006304)
MATSUZAWA Taiju Tohoku Univ., Res.Inst. for TB and Cancer, Prof., 抗酸菌病研究所, 教授 (10006108)
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| Project Period (FY) |
1987 – 1989
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| Keywords | Chemical Synthesis / Diagnosis / Radiopharmaceutical / PET / Positron / Labeled Sugar |
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| Research Abstract |
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.
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