2-(3-羟基-1-金刚烷基)-2-乙醛酸的合成 |
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引用本文: | 李靖柯,周鸿睿,彭俊,冯悦,胡湘南.2-(3-羟基-1-金刚烷基)-2-乙醛酸的合成[J].中国医药工业杂志,2012,43(4):251-253. |
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作者姓名: | 李靖柯 周鸿睿 彭俊 冯悦 胡湘南 |
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作者单位: | 重庆医科大学药学院,重庆,400016 |
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摘 要: | 金刚烷经相继甲酸化、酰氯化后与丙二酸二乙酯乙氧基镁反应,得到1-金刚烷甲酰基丙二酸二乙酯,再经水解脱羧、高锰酸钾氧化得到沙克列汀中间体2-(3-羟基-1-金刚烷基)-2-乙醛酸,总收率约28%。
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关 键 词: | 2-(3-羟基-1-金刚烷基)-2-乙醛酸 沙克列汀 2型糖尿病 中间体 合成 |
Synthesis of 2- (3-Hydroxy- 1-adamantyl) -2-glyoxylic Acid |
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Authors: | LI Jingke ZHOU Hongrui PENG Jun FENG Yue HU Xiangnan |
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Affiliation: | *(School of Pharmacy,Chongqing Medical University,Chongqing 400016) |
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Abstract: | 2-(3-Hydroxy-1-adamantyl)-2-glyoxylic acid,the intermediate of saxagliptin,was synthesized from adamantane via successive reactions with formic acid,thionyl chloride and diethyl ethoxymagnesium malonate to give diethyl 1-adamantaneformyl malonate,which was subjected to hydrolysis and decarboxylation by mixed acid and then oxidation by potassium permanganate.The overall yield was about 28%. |
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Keywords: | 2-(3-hydroxy-1-adamantyl)-2-glyoxylic acid saxagliptin type 2 diabetes intermediate synthesis |
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