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【结 构 式】 
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【药物名称】AZB-002 【化学名称】1-Methyl-2-(2-phenylethynyl)-3-(3-phenyl-2-propynyl)-3H-benzimidazol-1-ium tetrafluoroborate 【CA登记号】255716-41-7, 255716-40-6 (free base) 【 分 子 式 】C25H19BF4N2 【 分 子 量 】434.24818 |
【开发单位】University of Texas System (Originator) 【药理作用】ONCOLYTIC DRUGS, DNA-Damaging Drugs |
合成路线1
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.
| 【1】 Kerwin, S.M.; et al.; DNA cleavage chemistry of 1-methyl-2-phenylethynyl-3-(prop-2-ynyl)-3H-benzoimidazolium salts. 222nd ACS Natl Meet (Aug 26 2001, Chicago) 2001, Abst MEDI 146. |
| 【2】 David, W.M.; et al.; Synthesis of a heterocyclic aza-enediyne and its DNA-cleavage properties. Bioorg Med Chem Lett 2000, 10, 22, 2509. |
| 【3】 Kerwin, S.M.; David, W. (Research Development Foundation ; University of Texas System); Novel DNA-cleaving antitumor agents. EP 1109552; US 6297284; WO 0003709; WO 0170217 . |
Extended Information