| Project/Area Number |
05670760
|
|---|
| Research Category |
Grant-in-Aid for General Scientific Research (C)
|
| Allocation Type | Single-year Grants |
|---|
| Research Field |
Radiation science
|
|---|
| Research Institution | Tohoku University |
|---|
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)
|
|---|
| 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)
高橋 俊博 東北大学, サイクロトロンRIセンター, 助手 (70143039)
|
|---|
| Project Period (FY) |
1993 – 1994
|
| Project Status |
Completed (Fiscal Year 1994)
|
| Budget Amount *help |
¥1,600,000 (Direct Cost: ¥1,600,000)
Fiscal Year 1994: ¥1,000,000 (Direct Cost: ¥1,000,000)
Fiscal Year 1993: ¥600,000 (Direct Cost: ¥600,000)
|
|---|
| Keywords | PET / On-column labelling / Automated synthesis / Positron-emitter / Radiopharmaceutical |
|---|
| 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.
|
