An investigation on stereospecific fluorination at the 2′-arabino-position of a pyrimidine nucleoside: radiosynthesis of 2′-deoxy-2′-[18F]fluoro-5-methyl-1-β-D-arabinofuranosyluracil

TETRAHEDRON

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Article

Alauddin, Mian M.¹ 

[1] Univ Texas MD Anderson Canc Ctr, Dept Expt Diagnost Imaging, Unit 59, Houston, TX 77030 USA

关键词: Stereospecific fluorination;    Fluorine-18;    Pyrimidine nucleoside;    PET;   

DOI  :  10.1016/j.tet.2012.10.001

来源: Elsevier

【 摘 要 】

Direct fluorination at the 2'-arabino-position of a pyrimidine nucleoside has been a long-standing challenge, yet we recently reported such a stereospecific fluorination for the first time in the synthesis of [F-18]FMAU, albeit in low yields. Herein we report the results of an investigation on stereospecific fluorination on a variety of precursors for synthesis of [F-18]FMAU. Several precursors were synthesized in multiple steps and fluorination was performed at the 2'-arabino-position using K[F-18]/kryptofix 2.2.2. All precursors produced [F-18]FMAU in low yields. (C) 2012 Published by Elsevier Ltd.

【 授权许可】

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