一锅法合成吡唑并[3,4-b]喹啉酮类化合物

目的:探究吡唑并[3,4-b]喹啉酮类化合物{Pyrazolo[3,4-b]quinolinone compounds,PQO}绿色、高效的合成方法。方法:以5-氨基-3-甲基-1-苯基吡唑、1,3-环己二酮类和苯乙二醛类水合物为原料,通过一锅法3组分反应合成PQO。结果:获得PQO的最佳合成工艺为EtOH/H_(2)O(V=1/1)为溶剂,反应温度50℃,反应时间1.5 h,且目标化合物经^(1)H NMR、^(13)C NMR和HR-MS确证。结论:该方法具有操作简单、产率高、高原子经济性等特点,在新药设计与合成、组合化学和天然产物合成中具有潜在的应用价值。

Synthesis, Characterization and Antibacterial Activities Study of a Pharmaceutical Cocrystal of Artesunate and 4,4’-Bipyridine

We report here a cocrystal with artesunate as the active pharmaceutical ingredient(API)and a pharmaceutical intermediate 4,4?-bipyridine as the cocrystal former(CCF).The analysis of single-crystal X-ray diffraction demonstrates that the eutectic structural unit consists of two artesunate molecules and one 4,4?-bipyridine molecule with their ratio to be 2:1.The carboxyl group on artesunate acts as a donor,and the acceptor is N on 4,4?-bipyridine,forming an O–H···N hydrogen bond.The appearance of new diffraction peaks in the X-ray powder diffraction pattern also indicates the formation of new phases.The PXRD results indicated a pure phase for the synthesized sample.The cocrystal is slightly soluble in water.Antimicrobial activities showed that the cocrystal displayed effective inhibition of different bacteria.