【药物名称】
化学结构式(Chemical Structure):
参考文献No.577373
标题:5'-[2-(2-Nitrophenyl)-2-methylpropionyl]-2'-deoxy-5-fluorouridine as a potential bioreductively activated prodrug of FUDR: Synthesis, stability and reductive activation
作者:Hu, L.; Liu, B.; Hacking, D.R.
来源:Bioorg Med Chem Lett 2000,10(8),797
合成路线图解说明:

Esterification of 2-nitrophenylacetic acid (I) with SOCl2 in MeOH produced methyl ester (II). Subsequent dialkylation of (II) using methyl iodide and NaH in the presence of 18-crown-6 gave methyl 2-nitrophenyl-2-methylpropionate (III), which was hydrolyzed to carboxylic acid (IV) with NaOH in MeOH. Finally, chemoselective acylation of the primery hydroxy group of 5-fluoro-2'-deoxyuridine (V) with (IV) under Mitsunobu conditions yielded the title ester.

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