Synthesis of C11-labelled heterocyclic compounds and analysis of those pharmacokinetics

2021 Fiscal Year Final Research Report

• Project/Area Number: 17K10383
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: National Institutes for Quantum Science and Technology
• Principal Investigator: ISHII HIDEKI 国立研究開発法人量子科学技術研究開発機構, 量子医科学研究所 先進核医学基盤研究部, 主任研究員 (80425610)
• Project Period (FY): 2017-04-01 – 2022-03-31
• Keywords: 炭素11 / PET / イミダゾリン環 / 11C一酸化炭素 / ルイス酸

Outline of Final Research Achievements

Lewis acid mediated transformation of 11C-methyl esters to heterocycles has investigated. Firstly, we succeeded the construction of imidazoline by reaction with 11C-methyl ester and ethylenediamine in the presence of trimethyl aluminum as a Lewis acid (AlMe3). However after worked up of the reaction, AlMe3 generated large amount of insoluble matter which is difficult to purify imidazoline using auto-synthesizer. Thus, we examined another Lewis acids. Finally, we found that titanium-based Lewis acid is worked well to give good yield of imidazolines and to generate much less amount of insoluble matter.

Free Research Field

有機合成化学

Academic Significance and Societal Importance of the Research Achievements

本研究成果はエステル基を簡便にヘテロ環に変換する手法の開発であり、チタン系化合物を用いた変換反応はこれまで報告例がなく新規の手法の開発として学術的な意義は高いと言える。また本手法は炭素11標識エステル類を簡便にヘテロ環に変換するものであり、今後本手法を用いた新規のＰＥＴプローブの開発が大いに期待され、診断や治療に役立つＰＥＴプローブの開発にも貢献することが期待でき社会的意義は大きいと考えられる。