1994 Fiscal Year Final Research Report Summary
Development of the on-column labelling method for automated preparation of radiopharmaceuticals for PET study
| Project/Area Number |
05670760
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| Research Category |
Grant-in-Aid for General Scientific Research (C)
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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 |
IWATA Ren Cyclotron and Radioisotope Center, Tohoku University Associate Professor, サイクロトロンRIセンター, 助教授 (60143038)
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| Co-Investigator(Kenkyū-buntansha) |
TADA Masao Institute for Development, Aging and Cancer Associate Professor, 加齢医学研究所, 助教授 (10006083)
IDO Tatsuo Cyclotron and Radioisotope Center, Tohoku University Professor, サイクロトロンRIセンター, 教授 (80134063)
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| Project Period (FY) |
1993 – 1994
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| Keywords | PET / On-column labelling / Automated synthesis / Positron-emitter / Radiopharmaceutical |
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| Research Abstract |
A new, convenient on-column method using kieselguhr has been developed for the automated preparations of [<@D111@>D1C] fatty acids and [<@D111@>D1C] amino acids The reaction of [<@D111@>D1C] carbon dioxide with a Grignard reagent and purification by liquid-liquid extraction were carried out in a liquid layr supported by a commercially available kieselauhr, Extrelut<@D1(]SY.encircledR.[)@>D1 (Merck). [<@D111@>D1C] Carbon dioxide was efficiently trapped into a reagent solution kept by an Extrelut column and the free [<@D111@>D1C] fatty acid formed by quenching with dil. HCl was sequentially extracted by flowing an appropriate organic solvent from the reaction column into the solvent and then from the solvent into a short column of Extrelut for [<@D111@>D1C] acetic acid or silica gel for [<@D111@>D1C] palmitic acid. [<@D11@>D1C] Acetic acid was prepared in over 90% radiochemical yield and [<@D111@>D1C] palmitic acid in approx. 50% radiochemical yield, within 15 min, with the same system and procedure.
The on-column synthesis of 1-aminocyclopentane-1-[^<11>C] carboxylic acid ( [^<11>C] ACPC) from [^<11>C] HCN was also carried out. The whole synthetic procedure, including the trapping and reaction of [^<11>C] HCN as well as the following extraction and acid hydrolysis, was remarkably simplified, and the preparation has been successfully accommodated to routine production of [^<11>C] ACPC.The established method provides radiochemically pure [^<11>C] ACPC in over 60% radiochemical yield within 40 min after the end of bombardment.
Thus, the present study has demonstrated that the on-column labelling based on column extraction can simplify synthetic procedures for the preparation of PET radiopoharmaceuticals and facilitate automation for routine use in PET.
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