河北师范大学学报—

期刊信息

刊名：河北师范大学学报（自然科学版）Journal of Hebei Normal University (Natural Science)
主办：河北师范大学
ISSN： 1000-5854
CN： 13-1061/N
中国科技核心期刊
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中国高校优秀科技期刊
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沙格列汀及其差向异构体的构型研究

孙艳美¹

张勇¹

曹文婷¹

王秋艳¹

原现瑞²

1. 河北科技大学化学与制药工程学院, 河北石家庄 050018;
2. 河北科技大学分析测试中心, 河北石家庄 050018
DOI： 10.13763/j.cnki.jhebnu.nse.2017.01.010

Study on the Configuration of Saxagliptin and It's Epimerides

SUN Yanmei¹, ZHANG Yong¹, CAO Wenting¹, WANG Qiuyan¹, YUAN Xianrui²

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摘要/Abstract

摘要：

参考文献方法合成了沙格列汀及其3种差向异构体，通过红外光谱（FTIR）和多种1D和2D NMR实验确认了它们的化学结构，包括¹H，¹³C，DEPT90，DEPT135，¹H-¹HCOSY，HSQC和HMBC实验等.进行了沙格列汀及3种差向异构体的2D NOESY实验，得到其分子内NOE数据，研究这些NOE实验结果，分别证实了它们的立体构型.培养了沙格列汀的晶体，其单晶X射线衍射实验结果与核磁共振实验结果相符合，沙格列汀晶体构型、溶液构型（NMR实验结果）和沙格列汀结合受体蛋白的构型是一致的.

Abstract：

Saxagliptin and it's three epimerides were synthesized according to the reported literatures.The chemical structures of these compounds were confirmed through FT-IR,1D and 2D NMR spectroscopies.These experiments included ¹H,¹³C,DEPT90,DEPT135,¹H-¹H COSY,HSQC and HMBC etc.Their configurations were verified using NOE results obtained NMR NOESY experiments.The crystal structure of saxagliptin from X-ray diffraction experiment matched well with the configuration from NMR experiments.The configurations of saxagliptin of crystal form,in solution and after binding to its protein acceptor were same.

关键词

关键词： 沙格列汀 ; NOE实验 ; 立体构型 ; 差向异构体

Key words： saxagliptin ; NOE results ; configuration ; epimerides

参考文献 9

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