Synthesis of [18F]GBR 12909, a dopamine reuptake inhibitor
Synthesis of [18F]GBR 12909, a dopamine reuptake inhibitor
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多巴胺再摄取抑制剂[18F]GBR 12909的合成
DOI：
10.1002/jlcr.2580280708
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发表时间：
1990
影响因子：
1.8
通讯作者：
M. Kilbourn
中科院分区：
文献类型：
--
作者：
M. Haka;M. Kilbourn
Preparation of no-carrier-added fluorine-18 labeled GBR 12909 (1-[2-(bis(4-fluorophenyl)methoxy)ethyl]-4-(3-phenylpropyl)piperazine), a specific and high affinity inhibitor of dopamine reuptake, is described. 4-Fluoro-4′-[18F]fluorobenzophenone was prepared by [18F]fluoride ion substitution of the corresponding trimethylammonium trifluoromethanesulfonate salt. The [18F]benzophenone was reduced to the benzhydrol, chlorinated, then used to alkylate 1-(2-hydroxyethyl)-4-(3-phenyl-propyl)piperazine to yield [18F]GBR 12909 in high specific activity (≥2000 Ci/mmol) and overall yields of 10–16% (corrected, 140 min synthesis).
