Radiosynthesis of 3′-deoxy-3′-[18F]fluorothymidine:: [18F]FLT for imaging of cellular proliferation in vivo

Radiosynthesis of 3′-deoxy-3′-[18F]fluorothymidine:: [18F]FLT for imaging of cellular proliferation in vivo
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DOI:
10.1016/s0969-8051(99)00104-3
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发表时间:
2000-02-01
影响因子:
3.1
通讯作者:
Shields, AF
Shields, AF
中科院分区:
医学4区
文献类型:
--
作者:
Grierson, JR;Shields, AF

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基于[F-18]氟化物取代受保护的硝基苯磺酸盐前体,发展了一种可靠的放射合成3 '-脱氧-3'-[F-18]氟胸苷([F-18]FLT)的方法。描述了一种简单的三步合成,其可用于制备>10 mCi(370 MBq)的放射化学纯的[F-18]FLT,在100分钟内在EOS下具有>1 Ci/μ mol(37 GBq/μ mol)的比活度,并且具有13%的放射化学产率,轰击倾向(EOB); 7%的合成终止(EOS)。[F-18]FLT已被设计为一种新的正电子发射断层扫描成像剂,用于基于胸苷代谢在体内可视化细胞增殖。核医学生物学27;2:143-156,2000。(C)2000 Elsevier Science Inc. All rights reserved.
A reliable radiosynthesis of 3'-deoxy-3'-[F-18]fluorothymidine ([F-18]FLT) has been developed based on [F-18]fluoride displacement of a protected nosylate precursor. A simple three-step synthesis is described that is useful for preparing >10 mCi (370 MBq) of radiochemically pure [F-18]FLT, with a specific activity >1 Ci/mu mol (37 GBq/mu mol) at EOS within 100 min and in 13% radiochemical yield tend of bombardment (EOB); 7% end of synthesis (EOS). [F-18]FLT has been designed as a new positron emission tomography imaging agent for visualizing cellular proliferation in vivo based on the metabolism of thymidine. NUCL MED BIOL 27;2:143-156, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.