五种喹噁啉-1,4-脱二氧化合物的合成

Synthesis of Five 1,4-bisdesoxyquinoxaline

喹噁啉-1,4-二氧类化合物(QdNOs)具有抗菌和促动物生长的作用,其在动物体内代谢可产生喹噁啉-1,4-脱二氧化合物。为深入了解喹噁啉-1,4-脱二氧化合物在动物体内的残留、代谢及毒理,对五种喹噁啉-1,4-二氧化合物的脱二氧代谢产物进行了半合成研究,以提供受试物标准品。文章探讨了反应溶剂、不同碱体系,反应物物质的量等对产物收率的影响,结果显示,最优条件下,五种脱二氧代谢产物的收率在72.5%~86.1%之间。五种产物的结构利用核磁共振氢谱和质谱进行了分析和表征。

Quinoxaline-1,4-dioxides(QdNOs)are antibacterial agents used as growth promoters in animal husbandry,and their animal vivo metabolism can produce 1,4-bisdesoxyquinoxaline.To further study the residue,the metabolism and toxicology of QdNOs,a semi-synthetic of five 1,4-bisdesoxyquinoxaline compounds are carried out in this paper.The conditions of reaction solvent,the alkali,the amount of the alkali and the ratio of the reactant are valuated.Under the optimized conditions,the product yield of five 1,4-bisdesoxyquinoxaline ranged from 72.5%to 86.1%.All synthesized compounds are characterized by 1H NMR and ESI-MS.