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【结 构 式】 
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【药物名称】Crisnatol mesilate, 770U82 mesylate, BW-A770U mesylate 【化学名称】2-[(6-Chrysenylmethyl)amino]-2-methyl-1,3-propanediol methanesulfonate 【CA登记号】96389-69-4, 96389-68-3 (free base), 96404-70-5 (HCl) 【 分 子 式 】C24H27NO5S 【 分 子 量 】441.55049 |
【开发单位】GlaxoSmithKline (Originator), Ilex Oncology (Licensee), Janssen (Licensee), Sanofi-synthélabo (Licensee) 【药理作用】DNA Topoisomerase II Inhibitors, DNA-Intercalating Drugs |
合成路线1
The formylation of chrysene (I) with dichloromethyl methyl ether by means of SnCl4 in o-dichlorobenzene gives chrysene-6-carboxaldehyde (II), which is then reductocondensed with 2-amino-2-methylpropane-1,3-diol (III) by means of p-toluenesulfonic acid in refluxing toluene, followed by dilution with ethanol and reduction with sodium cyanoborohydride.
| 【1】 Bair, K.W. (Glaxo Wellcome plc); Polycyclic aromatic cpds. EP 0125702; US 4719047 . |
| 【2】 Bair, K.W. (Glaxo Wellcome plc); Polycyclic biocidal cpds., their synthesis, formulations containing them. EP 0182609; ES 8706102; ES 8802415; ES 8802481 . |
| 【3】 Andrews, C.W.; Tuttle, R.L.; Cory, M.; McKee, D.D.; Bair, K.W.; Knick, V.C.; 2-[(Arylmethyl)amino]-2-methyl-1,3-propanediol DNA intercalators. An examination of the effects of aromatic ring variation on antitumor activity and DNA binding. J Med Chem 1991, 34, 7, 1983-90. |
| 【4】 Castaner, J.; Prous, J.; Crisnatol Mesylate. Drugs Fut 1993, 18, 3, 216. |