快速微波辅助氟化反应合成新型5'-脱氧-5'-氟尿苷衍生物。
Rapid microwave-assisted fluorination yielding novel 5'-deoxy-5'-fluorouridine derivatives.
作者信息
Le H Phuoc, Müller Christa E
机构信息
Pharmaceutical Sciences Bonn (PSB), Pharmaceutical Chemistry, Institute of Pharmacy, University of Bonn, Kreuzbergweg 26, 53115 Bonn, Germany.
出版信息
Bioorg Med Chem Lett. 2006 Dec 1;16(23):6139-42. doi: 10.1016/j.bmcl.2006.08.093. Epub 2006 Sep 7.
The preparation of (18)F-labeled ligands for positron emission tomography (PET) and the subsequent imaging have to be completed within a half-life of the neutron-deficient isotope ((18)F=110 min). In this paper, we report a rapid fluorination approach to obtain 5'-deoxy-5'-fluoro-substituted uracil nucleoside analogues. Nucleophilic substitution at the 5'-position of the nucleosides was achieved within 45 min providing excellent yields of 75-92% by application of microwaves.
用于正电子发射断层扫描（PET）的（18）F标记配体的制备以及后续成像必须在缺中子同位素（（18）F = 110分钟）的半衰期内完成。在本文中，我们报道了一种快速氟化方法来获得5'-脱氧-5'-氟取代的尿嘧啶核苷类似物。通过微波辐射，核苷5'-位的亲核取代反应在45分钟内完成，产率高达75-92%。
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