Miazga A, Poopeiko N E, Piasek A, Siweckar M A, Kulikowski T
Institute of Biochemistry and Biophysics, Polish Academy of Sciences, Warszawa, Poland.
Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):805-7. doi: 10.1081/NCN-120022639.
Novel synthesis of 2',3'-dideoxy-3'-fluoro-2-thiothymidine (SFLT) based on transformation of appropriately protected 1-beta-D-threo-ribofuranosylthymine is presented. The synthesis and evaluation of SFLT 5'-O-ester prodrugs enzymatic hydrolysis, as well as their anti-HIV activity, is also described.
介绍了基于适当保护的1-β-D-苏型呋喃核糖基胸腺嘧啶转化的新型2',3'-二脱氧-3'-氟-2-硫代胸腺嘧啶（SFLT）合成方法。还描述了SFLT 5'-O-酯前药的合成、酶促水解评估及其抗HIV活性。
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