阿片受体显像剂<sup>11</sup>C-Carfentanil的前体合成及放射性标记

阿片受体显像剂¹¹C-Carfentanil的前体合成及放射性标记

摘要: 为合成μ阿片受体显像剂:1-（2-苯乙基）-4-（N-苯基丙酰胺基）哌啶-4-羧酸［¹¹C］甲酯（［¹¹C］-methyl 1-phenethyl-4-( N-phenylpropanamido)piperidine-4-carboxylate，¹¹C-CFN)，合成了标记前体：1-苯乙基-4-（N-苯基丙酰胺基）哌啶-4-羧酸，并用¹¹C标记。标记前体和各步合成中间体均经核磁和质谱确证。采用¹¹C-Triflate-CH₃标记，Sep-Pak柱色层纯化，标记率为(67.3±2.3)%(n=3)，产物放化纯度大于98%，比活度为1.67×10¹⁴Bq/g(66.6 PBq/mol)，基本满足临床研究的需求。

Abstract: The ［¹¹C］-methyl 1-phenethyl-4-(N-phenylpropanamido)piperidine-4-carboxylate (¹¹C-Carfentanil) as μ opiate receptor imaging agent and its precursor have been synthesized. The precursor has been confirmed by 1H NMR and MS. ¹¹C-Carfentanil was prepared without using HPLC purification. Labeling yields, radiochemistry purity and specific activity are (67.3±2.3)%(n=3), 98% and 1.67×10¹⁴Bq/g (66.6 PBq/mol) respectively.