阿片受体显像剂11C-Carfentanil的前体合成及放射性标记

摘要

The [11C]-methyl l-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. 67×1014 Bq/g (66. 6 PBq/mol) respectively.%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士2.3)％(n=3),产物放化纯度大于98％,比活度为1.67×1014 Bq/g(66.6 PBq/mol),基本满足临床研究的需求.