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本文报道以色胺1a或5-甲氧基色胺盐酸盐1b为原料,用相应二羧酸酸氯进行酸化得到六个相应的双-色胺-Nb,Nb-酰胺2,继而经Bischler-Naieralski环合反应得到六个双-3,4-二氯-β-琳3,再经Pd/C催化脱氢得到六个双β-啉化合物4。设计合成的12个(二氢)-β-啉化合物均未见文献报道。经初步体外抗白血病株L1210试验结果表明,双β-啉化合物4a,4b及4f均具一定的抑制活性,值得作进一步研究。
This article reports that serotonin 1a or 5-methoxytryptamine hydrochloride 1b is used as the starting material and acidified with the corresponding dicarboxylic acid chloride to give six corresponding bis-tryptamine-Nb, Nb-amide 2, Naieralski cyclization to give six bis-3,4-dichloro-β-Lin 3, followed by catalytic dehydrogenation of Pd / C to give six bis-4 compounds. None of the 12 (dihydro) -β-oxo compounds designed and synthesized have been reported in the literature. The preliminary in vitro anti-leukemia strain L1210 test results show that the two beta-4n compounds 4a, 4b and 4f have certain inhibitory activity, deserves further study.