新型喹诺酮类衍生物的合成与表征

Synthesis and Characterization of Novel Quinolone Derivatives

通过设计以喹啉酸和色胺类化合物为原料,经DCC和HOBT脱水缩合反应将两个具有抗肿瘤活性的药效团进行拼接,一步合成3-位含吲哚片段的新型喹诺酮衍生物。并将得到的目标化合物经1H-NMR、13C-NMR和质谱确证为3-位含吲哚片段的新型喹诺酮衍生物。3-位含吲哚片段的新型喹诺酮衍生物是一种具有潜在药理活性的新型喹诺酮衍生物,未见文献报道。为后续广泛合成3-位含吲哚片段的新型喹诺酮衍生物和开展药理活性研究提供物质基础。

We designed a novel quinolone derivative containing indoles in 3-site by combining two pharmacopharmacophores with antitumor activity through dehydration condensation reaction of DCC and HOBT using quinolinic acid and tamines as raw materials.The target compounds were confirmed by 1H-NMR,13C-NMR and mass spectrometry as novel quinolone derivatives containing indole fragments at 3-site.Novel quinolone derivatives containing indole fragments at 3-site are novel quinolone derivatives with potential pharmacological activity,which have not been reported in the literature.It provides material basis for the subsequent synthesis of novel quinolone derivatives containing 3-site indoles and the study of their pharmacological activities.