抗肿瘤吡咯三嗪类激酶抑制剂的合成

目的：设计与合成具有分子靶向性、低毒高效新型血管生成抑制剂类抗肿瘤药物吡咯三嗪.方法：以羟胺磺酸和2-吡咯甲醛为原料合成2,4-二氯吡咯2.1-f]1.2.4]三嗪,然后进一步胺化、催化氢化得到11个吡咯三嗪类衍生物.结果：合成的化合物及中间体均经过核磁共振氢谱与质谱进行了结构表征,确证结构与目标产物一致.结论：合成了11个抗肿瘤吡咯三嗪类激酶抑制剂,该合成方法可靠、质量可控,能用于抗肿瘤吡咯三嗪类激酶抑制剂的合成.

Synthesis of Pyrrolo [2.1-f] [1.2.4] triazine-like Kinase Inhibitor,A Kind of Anti-tumor Drug

Objective：To design and synthesize a novel molecular targeting angiogenesis inhibitor with anti-tumor activity and low toxicity.Methods：Hydroxylamine-O-sulfonic acid and pyrrole-2-carboxaldehyde were used as starting material to synthesize 2,4-Dichloropyrrolo2,1-f] 1,2,4] triazine,and then the products were aminated and catalytically hydrogenated to synthesize 11 kinds of pyrrolo triazine derivatives.Results：The structures of the synthesized compounds and intermediate products were identified by hydrogen nuclear magnetic resonance （1H NMR） and mass spectrometry （MS）,and confirmed to be the same with the target compounds.Conclusions：The synthetic route was simple,controllable and suitable for preparation of pyrrolo triazine-like kinase inhibitors,a kind of anti-tumor drug.