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

来源：

NUCLEAR MEDICINE AND BIOLOGY | 1993年 / 20卷 / 06期

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

页码：777 / 794

页数：18

共 56 条

[1] DISPLACEMENT OF A NITRO-GROUP BY [F-18]-LABELED FLUORIDE-ION - A NEW ROUTE TO ARYL FLUORIDES OF HIGH SPECIFIC ACTIVITY [J].