Rapid and reproducible radiosynthesis of [18F] FHBG
Rapid and reproducible radiosynthesis of [18F] FHBG
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DOI：
10.1016/s0969-8051(03)00096-9
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发表时间：
2004-01-01
影响因子：
3.1
通讯作者：
Welch, MJ
中科院分区：
文献类型：
--
作者：
Ponde, DE;Dence, CS;Welch, MJ
采用一锅法两步合成了PET基因治疗显像剂9-（4-[F-18] Fluoro-3-hydroxymethylbutyl）guanine（[F-18] FHBG）。微波（MW）介导的N-2，单甲氧基三苯甲基-9-[4-（甲苯磺酰基）-3-单甲氧基三苯甲基-甲基丁基]鸟嘌呤的亲核取代，使用无载体添加的[F-18]氟化物，随后用盐酸脱保护和HPLC纯化，得到[F-18] FHBG。放射化学产率（衰变校正）为12 +/- 5%（n = 35），合成时间为55-60 min，放射化学纯度> 99%。将该化合物用于肺成像，并注射到先前感染单纯疱疹病毒1型胸苷激酶（HSV 1-tk）报告基因的Sprague-Dawley大鼠中。MicroPET成像显示积聚局限于肺部。(C)2004爱思唯尔公司All rights reserved.
9-(4-[F-18] Fluoro-3-hydroxymethylbutyl) guanine ([F-18] FHBG), an imaging agent for gene therapy using PET, was prepared in a one-pot, two-step synthesis. Microwave (MW) mediated nucleophilic fluorination of N-2, monomethoxytrityl-9-[4-(tosyl)-3-monomethoxytrityl-methylbutyl] guanine using no-carrier-added [F-18] fluoride, followed by deprotection with hydrochloric acid and HPLC purification, gave [F-18] FHBG. The radiochemical yield (decay corrected) was 12 +/- 5% (n = 35), the synthesis time was 55-60 min, and the radiochemical purity was >99%. The compound was used for lung imaging and was injected into Sprague-Dawley rats previously infected with the herpes simplex virus type 1 thymidine kinase (HSV1-tk) reporter gene. MicroPET imaging showed accumulation confined to the lungs. (C) 2004 Elsevier Inc. All rights reserved.