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脱二氧乙酰甲喹及N4-脱一氧乙酰甲喹的合成及结构表征
引用本文:汤有志,远立国,沈祥广.脱二氧乙酰甲喹及N4-脱一氧乙酰甲喹的合成及结构表征[J].动物医学进展,2012(3):33-36.
作者姓名:汤有志  远立国  沈祥广
作者单位:华南农业大学兽医学院广东省兽药研制与安全评价重点实验室;华南农业大学兽医学院
基金项目:广东省自然科学基金(10451064201005477);广东高校优秀青年创新人才培育项目(LYM09032);华南农业大学校长基金(5500-K11046);大连三仪-华南农大科研基金
摘    要:乙酰甲喹属于喹喔啉-N,N-二氧化物类兽药,有研究认定3-甲基-2-乙酰基-喹喔啉是乙酰甲喹的残留标示物。N4-脱一氧乙酰甲喹则被认为是乙酰甲喹在大鼠、鸡及猪肝微粒体中的主要代谢产物。为给乙酰甲喹代谢产物及代谢机制的深入研究提供理论依据,本研究采用Na2S2O4还原乙酰甲喹,合成3-甲基-2-乙酰基-喹喔啉和N4-脱一氧乙酰甲喹,经质谱、红外及1 H核磁等光谱技术对二者的化学结构进行了确证,为乙酰甲喹代谢产物及代谢机制的深入研究提供了理论依据。

关 键 词:乙酰甲喹  3-甲基-2-乙酰基-喹喔啉  N4-脱一氧乙酰甲喹  代谢产物

Synthesis and Structure Confirmation of 3-methyl-2-acetyl-quinoxaline and 4-desoxymequindox
TANG You-zhi,YUAN Li-guo,SHEN Xiang-guang.Synthesis and Structure Confirmation of 3-methyl-2-acetyl-quinoxaline and 4-desoxymequindox[J].Progress In Veterinary Medicine,2012(3):33-36.
Authors:TANG You-zhi  YUAN Li-guo  SHEN Xiang-guang
Institution:1(1.Guangdong Provincial Key Laboratory of Veterinary Drugs’Research and Safety Evaluation,College of Veterinary Medicine,South China Agricultural University,Guangzhou,Guangdong,510642,China;2.College of Veterinary Medicine, South China Agricultural University,Guangzhou,Guangdong,510642,China)
Abstract:Mequindox is a quinoxaline-N,N-dioxide used in veterinary medicine.3-methyl-2-acetyl-quinoxaline was identified as the marker residue of mequindox.4-desoxymequindox is proved to be the main metabolite of mequindox in liver microsomes of rat,chicken and pig.In order to provide valuable information to the study of metabolites and the mechanism of mequindox,3-methyl-2-acetyl-quinoxaline and 4-desoxymequindox was prepared through reducing mequindox with Na2S2O4 in this work.The chemical structures of these two compounds were identified by ESI-MS,IR,1H-NMR.This finding will provide valuable information to the study of metabolites and the metabolic mechanism of mequindox.
Keywords:mequindox  3-methyl-2-acetyl-quinoxaline  4-desoxymequindox  metabolite
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