【药物名称】AZB-002
化学结构式(Chemical Structure):
参考文献No.41925
标题:Novel DNA-cleaving antitumor agents
作者:Kerwin, S.M.; David, W. (Research Development Foundation ; University of Texas System)
来源:EP 1109552; US 6297284; WO 0003709; WO 0170217
合成路线图解说明:

Phenylenediamine (I) was condensed with phenylpropargyl aldehyde (II) in the presence of formic acid to generate the benzimidazole derivative (III). Subsequent N-alkylation of (III) with trimethyloxonium tetrafluoroborate gave the title benzimidazolium salt.

参考文献No.599874
标题:Synthesis of a heterocyclic aza-enediyne and its DNA-cleavage properties
作者:David, W.M.; Kumar, D.; Kerwin, S.M.
来源:Bioorg Med Chem Lett 2000,10(22),2509
合成路线图解说明:

Phenylenediamine (I) was condensed with phenylpropargyl aldehyde (II) in the presence of formic acid to generate the benzimidazole derivative (III). Subsequent N-alkylation of (III) with trimethyloxonium tetrafluoroborate gave the title benzimidazolium salt.

参考文献No.630338
标题:DNA cleavage chemistry of 1-methyl-2-phenylethynyl-3-(prop-2-ynyl)-3H-benzoimidazolium salts
作者:Kerwin, S.M.; et al.
来源:222nd ACS Natl Meet (Aug 26 2001, Chicago) 2001,Abst MEDI 146
合成路线图解说明:

Phenylenediamine (I) was condensed with phenylpropargyl aldehyde (II) in the presence of formic acid to generate the benzimidazole derivative (III). Subsequent N-alkylation of (III) with trimethyloxonium tetrafluoroborate gave the title benzimidazolium salt.

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