AZB-002
Chemical Name: 1-Methyl-2-(2-phenylethynyl)-3-(3-phenyl-2-propynyl)-3H-benzimidazol-1-ium tetrafluoroborate
CAS No. 255716-41-7, 255716-40-6 (free base)
项目整合开发状态: Preclinical
项目研究机构: University of Texas System (Originator)
合成路线: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.
📌 参考资料/链接：
参考文献标题:Novel DNA-cleaving antitumor agents
文献作者:Kerwin,S.M.; David,W.(Research Development Foundation ; University of Texas System)
参考来源:EP 1109552; US 6297284; WO 0003709; WO 0170217
📄 详细内容
合成路线: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.
参考文献标题:Synthesis of a heterocyclic aza-enediyne and its DNA-cleavage properties
文献作者:David,W.M.; Kumar,D.; Kerwin,S.M.
参考来源:Bioorg Med Chem Lett 2000,10(22),2509
合成路线: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.
参考文献标题:DNA cleavage chemistry of 1-methyl-2-phenylethynyl-3-(prop-2-ynyl)-3H-benzoimidazolium salts
文献作者:Kerwin,S.M.; et al.
参考来源:222nd ACS Natl Meet (Aug 26 2001,Chicago) 2001,Abst MEDI 146