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利拉利汀中4种杂质的合成
引用本文:彭嘉勋,唐平,翟诗圆,毛雨,陈建芳.利拉利汀中4种杂质的合成[J].江苏药学与临床研究,2019,27(4):249-252.
作者姓名:彭嘉勋  唐平  翟诗圆  毛雨  陈建芳
作者单位:湖南工程学院化学化工学院,湖南工程学院化学化工学院,湖南工程学院化学化工学院,湖南工程学院化学化工学院,湖南工程学院化学化工学院
基金项目:湖南省自然科学基金资助课题(2018JJ4049)
摘    要:目的:为了加强对抗糖尿病药物利拉利汀的质量控制,合成了与利拉利汀相关的5个化合物:A、B、C、D和E。方法:利拉利汀1经取代反应分别得到化合物A和B;利拉利汀1经加成反应得到化合物C;利拉利汀1经三步取代反应得到化合物D;利拉利汀1经多步取代反应得到化合物E。结果与结论:合成了5个化合物,经HPLC确证,其中化合物A、B、D、E分别对应杂质A、B、D、E,其中化合物C的结构有待进一步研究。

关 键 词:利拉利汀  杂质  合成
收稿时间:2018/10/10 0:00:00
修稿时间:2019/8/7 0:00:00

Synthesis of Four Impurities of Linagliptin
PENG Jia-xun,TANG Ping,ZHAI Shi-yuan,MAO Yu and CHEN Jian-fang.Synthesis of Four Impurities of Linagliptin[J].Jiangsu Pharmacertical and Clinical Research,2019,27(4):249-252.
Authors:PENG Jia-xun  TANG Ping  ZHAI Shi-yuan  MAO Yu and CHEN Jian-fang
Institution:School of Chemistry and Chemical Engineering,Hunan Institute of Engineering,School of Chemistry and Chemical Engineering,Hunan Institute of Engineering,School of Chemistry and Chemical Engineering,Hunan Institute of Engineering,School of Chemistry and Chemical Engineering,Hunan Institute of Engineering,School of Chemistry and Chemical Engineering,Hunan Institute of Engineering
Abstract:Objective: In order to control the quality of oral antidiabetic linagliptin, five compounds related to linagliptin A, B, C, D and E were synthesized and characterized. Methods: The compound A and B were synthesized from linagliptin 1 via substitution reactions separately. The compound C was obtained from linagliptin 1 through an addition reaction. The compound D was prepared by three substitution reactions. The compound E was prepared by multiple substitution reactions. Results and Conclusions: The identities of A, B, D, E have been confirmed by HPLC were the imperities, but the identity of C needs further research.
Keywords:Linagliptin  Impurity  Synthesis
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