Elinafide mesilate, LU-79553, -Drug Synthesis Database

【结构式】

【药物名称】Elinafide mesilate, LU-79553

【化学名称】N,N'-Bis[2-(1,8-naphthalimido)ethyl]-1,3-diaminopropane dimethanesulfonate
　　　　　　N,N'-Bis[2-(1,3-dioxo-2,3-dihydro-1H-benz[de]isoquinolin-2-yl)ethyl]-1,3-diaminopropane dimethanesulfonate
　　　　　　2,2'-Propane-1,3-diylbis(iminoethylene)bis(2,3-dihydro-1H-benz[de]isoquinoline-1,3-dione) dimethanesulfonate

【CA登记号】162706-56-1 (acetate), 162706-37-8 (free base), 162706-57-2 (mesylate), 189336-92-3 (monoacetate), 189336-91-2 (monomesylate)

【分子式】C₃₃H₃₆N₄O₁₀S₂

【分子量】712.80367

【开发单位】Abbott (Originator)

【药理作用】Oncolytic Drugs, DNA-Intercalating Drugs

合成路线1

By condensation of 1,8-naphthalic anhydride (I) wih N,N’-bis(2-aminoethyl)propane-1,2-diamine (II) in refluxing dioxane, or in hot NMM.

参考文献中间体

【1】 Brana, M.F.; et al.; Bis-naphthalimides 3: Synthesis and antitumor activity of N,N'-bis[2-(1,8-naphthalimido)-ethyl]alkanediamines. Anti-Cancer Drug Des 1996, 11, 4, 297.
【2】 Keilhauer, G.; Romerdahl, C.; Brana, M.F.; Qian, X.-D.; Bousquet, P.; Castellano Berlanga, J.M.; Moran Moset, M.; Perez De Vega, M.J. (BASF AG); New bis-naphthalimides for the treatment of cancer. EP 0714387; JP 1997501662; US 5616589; WO 9505365 .
【3】 Koser, S.; Viergutz, W. (BASF AG); Method for producing aromatic bisimides. DE 19720803; WO 9852924 .

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	16982	1H,3H-benzo[de]isochromene-1,3-dione; 1,8-Naphthalic Anhydride	81-84-5	C₁₂H₆O₃	详情	详情
(II)	53968	1,4,8,11-Tetraazaundecane; 3,7-Diaza-1,9-nonanediamine; N,N'-Bis(2-aminoethyl)-1,3-propanediamine; N,N[-Bis(2-aminoethyl)-1,3-propanediamine	4741-99-5	C₇H₂₀N₄	详情	详情

Extended Information