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

被引:38
作者
MACH, RH
ELDER, ST
MORTON, TE
NOWAK, PA
EVORA, PH
SCRIPKO, JG
LUEDTKE, RR
UNSWORTH, CD
FILTZ, T
RAO, AV
MOLINOFF, PB
EHRENKAUFER, RLE
机构
[1] UNIV PENN, CEREBROVASC RES CTR, PHILADELPHIA, PA 19104 USA
[2] UNIV PENN, DEPT PHARMACOL, PHILADELPHIA, PA 19104 USA
关键词
D O I
10.1016/0969-8051(93)90165-Q
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
[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.
引用
收藏
页码:777 / 794
页数:18
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