摘要
目的 合成6个马来酸氯苯那敏有关物质,为其质量研究提供依据。方法 以卤代苯乙腈、卤代吡啶、N,N-二甲基氯乙烷为原料,通过亲核取代、脱氰基反应得到目标化合物N,N-二甲基-3-(2-氯苯基)-3-(2-吡啶基)丙胺(杂质A)、N,N-二甲基-3-(3-氯苯基)-3-(2-吡啶基)丙胺(杂质B)、N,N-二甲基-3-(4-氯苯基)-3-(3-吡啶基)丙胺(杂质C)、N,N-二甲基-3-(4-氯苯基)-3-(6-氯吡啶-2-基)丙胺(杂质D)、N,N-二甲基-3-(4-氯苯基)-3-(4-氯吡啶-2-基)丙胺(杂质E)和N,N-二甲基-3-(4-氯苯基)-3-(5-氯吡啶-2-基)丙胺(杂质F)。结果与结论上述有关物质的结构均经^(1)H-NMR、^(13)C-NMR和ESI-MS谱确证,本研究为制定马来酸氯苯那敏的质量标准提供了借鉴。
In order to control the quality of chlorpheniramine maleate, six related substances, named 3-(2-chlorophenyl)-N,N-dimethyl-3-(pyridin-2-yl)propan-1-amine(impurity A),3-(3-chlorophenyl)-N,N-dimethyl-3-(pyridin-2-yl)propan-1-amine(impurity B),3-(4-chlorophenyl)-N,N-dimethyl-3-(pyridin-3-yl)propan-1-amine(impurity C),3-(4-chlorophenyl)-3-(6-chloropyridin-2-yl)-N,N-dimethylpropan-1-amine(impurity D),3-(4-chlorophenyl)-3-(4-chloropyridin-2-yl)-N,N-dimethylpropan-1-amine(impurity E) and 3-(4-chlorophenyl)-3-(5-chloropyridin-2-yl)-N,N-dimethylpropan-1-amine(impurity F) were synthesized based on the synthetic process of chlorpheniramine maleate.The structures of the above related substances were confirmed by ^(1)H-NMR,^(13)C-NMR and ESI-MS.This study provided reference materials for the consistency evaluation of chlorpheniramine maleate.
作者
刘虎
朱文
宁鹏
禹曾达
LIU Hu;ZHU Wen;NING Peng;YU Zeng-da(Harvest(Hunan)Pharmaceutical Co.,Ltd.,Changsha 410200,China)
出处
《中国药物化学杂志》
CAS
CSCD
2022年第10期753-757,共5页
Chinese Journal of Medicinal Chemistry
关键词
氯苯那敏
有关物质
对氯苯乙腈
2-氯吡啶
chlorpheniramine
related substance
p-chlorobenzyl cyanide
2-chloropyridine
