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alpha-Difluoromethylornithine hydrochloride, Eflornithine hydrochloride, MDL-71782A, RMI-71782, DFMO, Vaniqa, Ornidyl

依氟鸟氨酸盐酸盐一水合物 依氟鸟氨酸 Chemical Name: 2-Difluoromethyl-DL-ornithine monohydrochloride monohydrate; 2-Difluoromethyl-2,5-diaminopentanoic acid monohydrochloride monohydrate
CAS No. 96020-91-6, 67037-37-0 (free base, anhydrous)
项目整合开发状态: Launched-1991
项目研究机构: Aventis Pharma (Originator), Bristol-Myers Squibb (Licensee), Gillette (Licensee), Ilex Oncology (Licensee), National Cancer Institute (Codevelopment), World Health Organization (Codevelopment)
合成路线:The optical resolution of 2,5-diamino-2-(difluoromethyl)pentanoic acid is performed as follows: The cyclization of its corresponding methyl ester (I) by means of sodium methoxide in methanol gives the racemic piperidone (II),which is submitted to optical resolution with (-)-binaphthylphosphoric acid yielding after crystallization and acidification with HCl the (+) and (-) piperidones (III) and (IV).Finally,both compounds are treated with refluxing 6N HCl to afford the target enantiomers.
📌 参考资料/链接：
参考文献标题:2-(Difluoromethyl)-2,5-diaminopentanoic acid
文献作者:Jung,M.; Bey,P.(Aventis Pharma SA)
参考来源:US 4413141

📄 详细内容


合成路线:By reaction of N2,N5-dibenzylidinolysine methly ester (I),with chlorodifluoromethane (II) in the presence of lithium diisopropylamide,followed by acid hydrolysis of the ester.Isolated as the monohydrochloride salt,monohydrate.

参考文献标题:D,L-alpha-Difluoromethyl ornithine
文献作者:Castar,J.; Blancafort,P.; Serradell,M.N.
参考来源:Drugs Fut 1981,6(3),142


合成路线:By reaction of N2,N5-dibenzylidinolysine methly ester (I),with chlorodifluoromethane (II) in the presence of lithium diisopropylamide,followed by acid hydrolysis of the ester.Isolated as the monohydrochloride salt,monohydrate.

参考文献标题:D,L-alpha-Difluoromethyl ornithine-RMI 71782
文献作者:Schijvenaars,M.; Franke,B.; Mariman,E.C.M.; Steegers-Theunissen,R.; Willemen,J.; Groenen,P.; Klootwijk,R.; Hol,F.
参考来源:Product data sheet,Centre de recherche Merrell,Strasbourg Cedex 2002,Abst 1027


合成路线:By reaction of N2,N5-dibenzylidinolysine methly ester (I),with chlorodifluoromethane (II) in the presence of lithium diisopropylamide,followed by acid hydrolysis of the ester.Isolated as the monohydrochloride salt,monohydrate.
参考文献标题:Catalytic irreversible inhibition of mammalial ornithine decarboxylase (E.C.4.1.1.17) by substrate and product analogues
文献作者:Metcalf,B.W.; et al.
参考来源:J Am Chem Soc 1978,1002551-53


产品链接: CAS No. 96020-91-6››

产品链接: CAS No.67037-37-0››
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