THE USE OF [F-18] 4-FLUOROBENZYL IODIDE (FBI) IN PET RADIOTRACER SYNTHESIS - MODEL ALKYLATION STUDIES AND ITS APPLICATION IN THE DESIGN OF DOPAMINE-D(1) AND DOPAMINE-D(2) RECEPTOR-BASED IMAGING AGENTS
THE USE OF [F-18] 4-FLUOROBENZYL IODIDE (FBI) IN PET RADIOTRACER SYNTHESIS - MODEL ALKYLATION STUDIES AND ITS APPLICATION IN THE DESIGN OF DOPAMINE-D(1) AND DOPAMINE-D(2) RECEPTOR-BASED IMAGING AGENTS
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DOI：
10.1016/0969-8051(93)90165-q
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发表时间：
1993-08-01
影响因子：
3.1
通讯作者：
EHRENKAUFER, RLE
中科院分区：
文献类型：
--
作者：
MACH, RH;ELDER, ST;EHRENKAUFER, RLE
制备了[F-18]4-氟苄基碘（[F-18]FBI），并进行了一系列模型烷基化研究，以确定其对不同亲核性的氮和硫亲核试剂的化学反应性。[F-18]FBI与仲胺和苯胺反应迅速，高产率地得到相应的N-[F-18]4-氟苄基类似物。酰胺和硫醇基团需要使用碱催化剂。通过研究基于多巴胺D1和D2受体的放射性示踪剂，证明了[F-18]FBI的效用。
[F-18]4-Fluorobenzyl iodide ([F-18]FBI) was prepared, and a series of model alkylation studies were conducted to determine its chemical reactivity toward nitrogen and sulfur nucleophiles of varying nucleophilicities. [F-18]FBI was found to react rapidly with secondary amines and anilines to give the corresponding N-[F-18]4-fluorobenzyl analogue in high yield. Amides and thiol groups required the use of a base catalyst. The utility of [F-18]FBI was documented by investigation of dopamine D1 and D2 receptor-based radiotracers.