【药物名称】Fiacitabine, FIAC
化学结构式(Chemical Structure):
参考文献No.68099
标题:FIAC
作者:Thorpe, P.J.; Casta馿r, J.
来源:Drugs Fut 1981,6(7),410
合成路线图解说明:

The reaction of 3-O-acetyl-5-O-benzoyl-2-deoxy-2-fluoro-D-arabinofuranosyl bromide (I) with tris(trimethylsilyl)cytosine (II) in methylene chloride gives 1-(3-O-acetyl-5-O-benzoyl-2-deoxy-2-fluoro-beta-D-arabinofuranosyl)cytosine (III), which is hydrolyzed by treatment with methanol NH3 to afford 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)cytosine (IV). Finally, this compound is iodinated by treatment with HIO3 - I2 in CCl4 - H2O - acetic acid.

参考文献No.607185
标题:Nucleosides. 110. Synthesis and antiherpes virus activity of some 2'-fluoro-2'-deoxyarabinofuranosylpyrimidine nucleosides
作者:Watanabe, K.A.; Reichman, U.; Hirota, K.; Lopez, C.; Fox, J.
来源:J Med Chem 1979,22(1),21-24
合成路线图解说明:

The reaction of 3-O-acetyl-5-O-benzoyl-2-deoxy-2-fluoro-D-arabinofuranosyl bromide (I) with tris(trimethylsilyl)cytosine (II) in methylene chloride gives 1-(3-O-acetyl-5-O-benzoyl-2-deoxy-2-fluoro-beta-D-arabinofuranosyl)cytosine (III), which is hydrolyzed by treatment with methanol NH3 to afford 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)cytosine (IV). Finally, this compound is iodinated by treatment with HIO3 - I2 in CCl4 - H2O - acetic acid.

合成路线图解说明:

FMAU is prepared by condensation of 3-O-benzoyl-2-fluoro-D-arabinosyl bromide (I) with trimethylsilylated thymine (II) followed by saponification of the protected nucleoside (III).

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