胆碱模块自动化合成^(11)C-carfentanil及Micro PET显像

Automated Synthesis of ^(11)C-carfentanil With ^(11)C-choline Module and Micro PET Imaging

为快速、高效合成中枢神经阿片受体显像剂11C-carfentanil(11C-CFN),对国产商业化11C-胆碱合成模块略做改动,并优化了合成条件。结果表明,采用4-哌啶乙酸钠,4-[(1-丙羰基)苯胺]-1-(2-苯乙基)[钠盐]作前体,DMSO作溶剂,11CH3-triflate作甲基化试剂,在胆碱模块上采用反应瓶法,可自动化合成11C-CFN。合成的11C-CFN活度>14.8 GBq、比活度>1.4×1014Bq/g、放化纯度>99%,校正合成效率>80%(n=55,以11CH3-triflate计算),全部合成时间为18 min。经Micro PET/CT证实,11C-CFN可用于μ阿片受体的PET显像研究。

A simple modified home-made 11C-choline module enabled to rapid and efficient synthesis 11C-carfenatnil（11C-CFN） as CNS μ-opioid receptor imaging agent.The synthesis of 11C-CFN was completed in a yield of 14.8 GBq within 18 min from 11C-CO2 on the choline module.The methylation took place from 4-piperidinecarboxylic acid,4-[（1-oxopropyl）phenylamino]-1-（2-phenylethyl）,sodium salt as precursor in DMSO solution.The radiochemical yields were over 80%（n=55,decay-corrected and based on 11CH3-triflate）.The radiochemical purity was over 95% and the specific activities was over 1.4×1014 Bq/g.The biologic activity of 11C-CFN was confirmed with Micro PET/CT imaging.