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吲哚生物碱deplancheine(1)具有在八氢吲哚并〔2,3-a〕喹嗪系统中C-3 E构型乙烯边链,而黄退热树碱flavopereirine(2),为体外癌症DNA合成抑制剂,已合成成功,但产率较低。作者在寻找合成吲哚类生物碱有效中间体过程中,发现3-乙酰-1,2,6,7,12,1 2b-六氢吲哚并〔2,3-a〕喹嗪-2-酮(5)为合成(1)(2)生物碱的理想中间体。目前已能通过改进法将3,4-二氢-β-咔啉(3)与羟甲烯基乙酰丙酮(4)缩合而迅速定量地获得(5)。(5)与1,2-乙二硫醇、对甲苯
The indole alkaloid deplancheine (1) has the C-3E-configuration vinyl side chain in the octahydroindolo [2,3-a] quinolizine system and the flavopereirine (2) for in vitro cancer DNA synthesis inhibitors, have been synthesized successfully, but the yield is low. In search of an effective intermediate for synthesis of indole alkaloids, the authors found that 3-acetyl-1,2,6,7,12,1 2b-hexahydroindolo [2,3-a] quinolizine- Ketone (5) is an ideal intermediate for the synthesis of (1) (2) alkaloids. (5) has been rapidly and quantitatively obtained by condensing 3,4-dihydro-β-carboline (3) with oxymethylacrylacetone (4) by a modification method. (5) with 1,2-ethanedithiol, p-toluene