同位素 ›› 2010, Vol. 23 ›› Issue (4): 230-234.DOI: 10.7538/tws.2010.23.04.0230

• 放射性药物和标记化合物 • 上一篇    下一篇

11C-CH3-Triflate甲基化法合成11C-PK11195

王明芳1;张锦明2;唐刚华3;李葆元1;高路1;罗志福4   

  1. 1. 南方医院 PET中心，广东 广州510515；2. 解放军总医院 核医学科，北京100853；3. 中山大学附属第一医院 核医学科，广东 广州510080；4. 中国原子能科学研究院 同位素研究所，北京102413
  • 收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2010-11-20 发布日期:2010-11-20

Radiosynthesis of 11C-PK11195 by Using [11C]Methyl Triflate

WANG Ming-fang1;ZHANG Jin-ming2;TANG Guang-hua3;LI Bao-yuan1;GAO Lu1;LUO Zhi-fu4   

  1. 1．PET Center, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China；2．Department of Nuclear Medicine, the PLA General Hospital, Beijing 100853, China；3．Department of Nuclear Medicine, First Affiliated Hospital of Sun Yat-sen University, Guangzhou 510080；4．Department of Isotope, China Institute of Atomic Energy, Beijing 102413, China
  • Received:1900-01-01 Revised:1900-01-01 Online:2010-11-20 Published:2010-11-20

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摘要： 利用11C-CH3-Triflate作为甲基化试剂，与去甲基前体1-(2-氯苯基)-N-(1-甲基丙基)-异喹啉-3-氨甲酰（nor-PK11195）进行甲基化反应合成N-[11C]甲基-N-(1-甲基丙基)-1-(2-氯苯基)异喹啉-3-氨甲酰（11C-PK11195），并建立了11C-PK11195的自动化合成方法。结果显示，以11C-CH3-Triflate为甲基化试剂合成11C-PK11195，在nor-PK11195用量为0.5~1.0 mg、反应温度90 ℃、反应时间5 min时，其标记率为51.7%±5.6％，11C-PK11195注射液的化学纯度和放化纯度均＞98%，比活度＞0.21 TBq/g。以上结果表明，11C-CH3-Triflate甲基化法可提高11C-PK11195标记率，缩短反应时间，降低前体用量；所制备的11C-PK11195注射液能够满足PET临床要求。

关键词: 11C-CH3-Triflate, 11C-PK11195, 自动化合成

Abstract: The purpose of this study was to establish a new synthetic method of 11C-PK11195. The automated radiosynthesis of 11C-PK11195 was accomplished by 11C-N-methylation of the corresponding desmethyl precursors (nor-PK11195) with 11C-methyl triflate (11C-CH3-Triflate) by the domestic-made synthesizer. The effects on labeling yield by N-methylation were evaluated. The results showed that the labeling yield of 11C-PK11195 was 51.7%±5.6％ under optimized synthesis conditions which were 0.5-1.0 mg nor-PK11195, 90 ℃ and 5 min. The radiochemical purity and chemical purity were higher than 98％, and the specific activity was above 0.21 TBq/g based on the HPLC UV analysis. 11C-PK11195 with a higher labeling yield can be prepared from the methylated reaction of 11C-CH3-Triflate with nor-PK11195. The results indicated that the 11C-N-methylation of nor-PK11195 with 11C-CH3-Triflate was an ideal synthetic method which required less nor-PK11195.

Key words: 11C-methyl triflate, 11C-PK11195, automated synthesis

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