ARYLTRIMETHYLAMMONIUM TRIFLUOROMETHANESULFONATES AS PRECURSORS TO ARYL [F-18] FLUORIDES - IMPROVED SYNTHESIS OF [F-18] GBR-13119
ARYLTRIMETHYLAMMONIUM TRIFLUOROMETHANESULFONATES AS PRECURSORS TO ARYL [F-18] FLUORIDES - IMPROVED SYNTHESIS OF [F-18] GBR-13119
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DOI：
10.1002/jlcr.2580270711
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发表时间：
1989-07-01
影响因子：
1.8
通讯作者：
TOORONGIAN, SA
中科院分区：
文献类型：
--
作者：
HAKA, MS;KILBOURN, MR;TOORONGIAN, SA
本文研究了三氟甲磺酸三甲基铵与[18 F]氟化物的芳香亲核取代反应。在45 - 165 ℃的温度范围内研究氟化。C，衰变校正产率范围为20- 80%。[18 F]GBR 13119，1-[2-{（4-[18 F]氟苯基）（苯基）甲氧基}乙基]-4-（3-苯基丙基）哌嗪，一种潜在的多巴胺摄取系统放射性示踪剂，已由4-N，N，N-三甲基苯胺苯基甲酮三氟甲磺酸盐制备成无载体添加形式。通过固相技术纯化得到产物，衰变校正的放射化学产率为20%，放射化学和化学纯度> 98%，无需HPLC。
Aromatic nucleophilic substitution of various trimethylammonium trifluoromethanesulfonates with [18F]fluoride has been evaluated. Fluorinations were studied over a temperature range of 45-165.degree. C, with decay corrected yields ranging from 20-80%. [18F]GBR 13119, 1-[2-{(4-[18F]fluorophenyl)(phenyl)methoxy}ethyl]-4-(3-phenylpropyl)piperazine, a potential radiotracer for the dopamine uptake system, has been prepared in no-carrier-added form from 4-N,N,N-trimethylaniliniumphenylmethanone trifluoromethanesulfonate. Purification by solid-phase techniques yielded the product in 20% decay corrected radiochemical yield and > 98% radiochemical and chemical purity without HPLC.