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Crisnatol mesilate, 770U82 mesylate, BW-A770U mesylate

克立那托 Chemical Name: 2-[(6-Chrysenylmethyl)amino]-2-methyl-1,3-propanediol methanesulfonate
CAS No. 96389-69-4, 96389-68-3 (free base), 96404-70-5 (HCl)
项目整合开发状态: Phase III
项目研究机构: GlaxoSmithKline (Originator), Ilex Oncology (Licensee), Janssen (Licensee), Sanofi-Aventis (Licensee)
合成路线: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.
📌 参考资料/链接:
参考文献标题:Polycyclic aromatic cpds
文献作者:Bair,K.W.(Glaxo Wellcome plc)
参考来源:EP 0125702; US 4719047

📄 详细内容


合成路线: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.

参考文献标题:Polycyclic biocidal cpds.,their synthesis,formulations containing them
文献作者:Bair,K.W.(Glaxo Wellcome plc)
参考来源:EP 0182609; ES 8706102; ES 8802415; ES 8802481


合成路线: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.

参考文献标题: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
文献作者:Bair,K.W.; Andrews,C.W.; Tuttle,R.L.; Knick,V.C.; Cory,M.; McKee,D.D.
参考来源:J Med Chem 1991,34(7),1983-90


合成路线: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.
参考文献标题:Crisnatol Mesylate
文献作者:Castar,J.; Prous,J.
参考来源:Drugs Fut 1993,18(3),216


产品链接: CAS No. 96389-69-4››

产品链接: CAS No.96389-68-3››