Department of Chemistry, National Taiwan Normal University , 88, Sec. 4, Ting-Chow Road, Taipei 116, Taiwan R.O.C.
J Org Chem. 2017 Feb 17;82(4):1961-1968. doi: 10.1021/acs.joc.6b02814. Epub 2017 Feb 8.
A concise route for the synthesis of indenoisoquinoline derivatives from 2-iodobenzamide and 1,3-indanedione derivatives in the presence of copper(II) chloride and cesium carbonate in acetonitrile solvent is reported. A wide variety of 2-iodobenzamide derivatives and indandiones could be used to synthesize indenoisoquinoline derivatives and other fused indenoisoquinoline in moderate to good yields. This methodology was adapted for the one-step synthesis of a series of clinically active topoisomerase I inhibitors such as NSC 314622, LMP-400, LMP-776.
本文报道了在氯化铜和碳酸铯存在下，由 2-碘苯甲酰胺和 1,3-茚二酮衍生物在乙腈溶剂中合成茚并异喹啉衍生物的简洁路线。该方法广泛适用于合成 2-碘苯甲酰胺衍生物和茚并二酮，以中等到良好的收率得到茚并异喹啉衍生物和其他稠合的茚并异喹啉。该方法适用于一系列临床活性拓扑异构酶 I 抑制剂如 NSC 314622、LMP-400、LMP-776 的一步法合成。
