Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.advisor | 조천규 | - |
dc.contributor.author | 이상주 | - |
dc.date.accessioned | 2020-04-13T16:41:23Z | - |
dc.date.available | 2020-04-13T16:41:23Z | - |
dc.date.issued | 2007-02 | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/149610 | - |
dc.identifier.uri | http://hanyang.dcollection.net/common/orgView/200000405539 | en_US |
dc.description.abstract | The aim of this study was to develop a method for the radiochemical synthesis of 3’-deoxy-3’-[18F]fluorothymidine ([18F]FLT) by nucleophilic substitution catalyzed by protic solvent. We introduced t-butanol (t-BuOH) as a new reaction solvent for the nucleophilic [18F]fluorination with [18F]fluoride using (5'-O-DMTr-2'-deoxy-3'-O-nosyl-ß-D-threo-pentofuranosyl)-3-N-BOC-thymine as a precursor to synthesis [18F]FLT. [18F]F- was eluted by 1) elution with tetrabutylammoniumbicarbonate (TBAHCO3), or 2) Cs2CO3 and kryptofix 2.2.2. (K222) after trapping of [18F]F- on ion exchange cartridge, or 3) addition of tetrabutylammonium hydroxide (TBAOH) and [18F]F- to the reactor without trapping of [18F]F- on ion exchange cartridge. We optimized the reaction conditions, and then applied them to automatic synthesis using commercially available radiochemistry modules (TracerLab MX and FX, GE Healthcare). We achieved a high radiochemical yield of 85.3±3.5% after hydrolysis on the radioTLC with TBAHCO3 as an elution solvent and 20 mg of precursor at 100oC. (n=4) With the same labeling condition, use of Cs2CO3 and K222 with t-BuOH and TBAOH with t-BuOH showed radiochemical yields of 57.1±22.5% and 55.0±18.8% on the radioTLC, respectively. (n=3 for each condition) Automated synthesis with TBAHCO3 as an elution solvent, and 20 mg of precursor at 120oC for 10 min [18F]fluorination showed radiochemical yields of 65.5±5.4% and 60.2±5.2% after HPLC purification with FX and MX modules, respectively. (n=10 for each condition) Synthesized [18F]FLT showed good stability for 6 hours. [18F]FLT was synthesized with high radiochemical yield by nucleophilic substitution catalyzed by protic solvent with mild reaction conditions and short preparation time. | - |
dc.publisher | 한양대학교 | - |
dc.title | Simple and Highly Efficient Synthesis of 3’-deoxy-3’-[18F]fluorothymidine by Nucleophilic Fluorination Catalyzed by Protic Solvent | - |
dc.type | Theses | - |
dc.contributor.googleauthor | 이상주 | - |
dc.contributor.alternativeauthor | Lee, Sang-Ju | - |
dc.sector.campus | S | - |
dc.sector.daehak | 대학원 | - |
dc.sector.department | 화학과 | - |
dc.description.degree | Master | - |
dc.contributor.affiliation | 유기합성 | - |
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