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美沙西汀-甲氧基-13C及其类似物的合成
引用本文:陈凯,代德胜,王春玲,魏翠雯,卿晶,沈桂富.美沙西汀-甲氧基-13C及其类似物的合成[J].同位素,2021,34(5):480.
作者姓名:陈凯  代德胜  王春玲  魏翠雯  卿晶  沈桂富
作者单位:深圳市中核海得威生物科技有限公司,广东 深圳518057
摘    要:美沙西汀-甲氧基-13C是一种最具潜力的标记底物,用于呼气检测肝功能。本研究以甲醇-13C为标记原料,通过Mitsunobu反应、官能团修饰高效合成了美沙西汀-甲氧基-13C,合成收率为63%,产品纯度>99%。同时应用该方法以甲醇-13C为标记原料合成了对甲氧基苯甲酸-甲氧基-13C,合成收率为67%,产品纯度>99%。建立的合成美沙西汀-甲氧基-13C的新方法可为呼气检测肝功能研究的开展提供参考。

关 键 词:甲醇-13C  美沙西汀-甲氧基-13C  对甲氧基苯甲酸-甲氧基-13C  Mitsunobu反应  

Synthesis of Methacetin-Methoxy-13C and its Analogue
CHEN Kai,DAI Desheng,WANG Chunling,WEI Cuiwen,QING Jing,SHEN Guifu.Synthesis of Methacetin-Methoxy-13C and its Analogue[J].Isotopes,2021,34(5):480.
Authors:CHEN Kai  DAI Desheng  WANG Chunling  WEI Cuiwen  QING Jing  SHEN Guifu
Affiliation:Shenzhen Zhonghe Headway Bio-Sci & Tech Co., Ltd., Shenzhen 518057, China
Abstract:In the current research on 13C-labeled compounds breath test of liver function, methacetin-methoxy-13C is the most potential substrate. To study a new method for synthesis methacetin-methoxy-13C, methanol-13C was used as the labeled material, methacetin-methoxy-13C was synthesized efficiently through Mitsunobu reaction and functional group modification. The synthesis yield was 63% and the chemical purity was above 99%. At the same time, this method was used to synthesize 4-methoxybenzoic acid-methoxy-13C with methanol-13C as the labeled material. The synthesis yield was 67% and the chemical purity was above 99%. The new scheme for the synthesis of methacetin-methoxy-13C with Mitsunobu reaction as the key reaction could provide a basis for the study of liver function by breath test.
Keywords:methanol-13C  methacetin-methoxy-13C  4-methoxybenzoic acid-methoxy-13C  Mitsunobu reaction  
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