【药物名称】Imidazoacridinone, Imidacrine, XLS-002, C-1311, Symadex
化学结构式(Chemical Structure):
参考文献No.369669
标题:Chromophore-modified antineoplastic imidazoacridinones. Synthesis and activity against murine leukemias
作者:Cholody, W.M.; Martelli, S.; Konopa, J.
来源:J Med Chem 1992,35(2),378-82
合成路线图解说明:

The synthetic procedure was carried out according to Cholody et al. (1). The starting 1-chloro-7-hydroxy-4-nitro-9(10H)-acridinone (I) was synthesized by the method of Capps (2). The condensation of (I) with 2-(diethylamino)ethylamine (II) in DMF gave 1-[2-(diethyl-amino)ethylamino]-7-hydroxy-4-nitro-9(10H)-acridinone (III) in good yield and purity. The reduction of the nitro group of (III) with hydrazine hydrate and Raney Ni in THF yielded the amino intermediate (IV), extremely unstable due to its sensitivity to oxidation, which was immediately used in the next step as crude hydrochloride salt. The salt (IV) was refluxed with 95% formic acid giving the imidazoacridinone derivative. The final product was isolated directly from the reaction mixture as hydrochloride salt after acidification with concentrated HCl and recrystalized from a mixture of methanol/acetone.

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