【药物名称】AU-254
化学结构式(Chemical Structure):
参考文献No.553716
标题:Synthesis and pharmacological profile of 1-aryl-3-substituted pyrrolo[3,2-c]quinolones
作者:Yum, E.K.; Kang, S.K.; Kim, S.S.; Choi, J.K.; Cheon, H.G.
来源:Bioorg Med Chem Lett 1999,9(19),2819
合成路线图解说明:

The title compound was prepared by two related ways from 3-iodo-8-methoxy-4-(2-methylphenyl)aminoquinoline (I). Alkylationof (I) with allyl bromide (II) and NaH afforded the N-allyl amine (III). Subsequent intramolecular palladium-catalyzed Heck reaction in (III) produced the title pyrroloquinoline. In an alternative procedure, the intermolecular palladium-catalyzed heteroannulation of (I) with 1-trimethylsilylpropyne (IV) gave the silyl pyrroloquinoline (V), which was finally desilylated by means of trifluoroacetic acid.

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