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| 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．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 |
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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.
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Received: 01 January 1900
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