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2-(3-羟基-1-金刚烷基)-2-乙醛酸的合成 被引量：4

Synthesis of 2-(3-Hydroxy-1-adamantyl)-2-glyoxylic Acid
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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%。 2-（3-Hydroxy-l-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 %.
作者 李靖柯 周鸿睿 彭俊 冯悦 胡湘南
机构地区 重庆医科大学药学院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2012年第4期251-253,共3页 Chinese Journal of Pharmaceuticals
基金 重庆市自然科学基金(2006BB5286)
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 2- （3-hydroxy-l-adamantyl） -2-glyoxylic acid saxagliptin type 2 diabetes intermediate synthesis
分类号 O624.5 [理学—有机化学]
  • 相关文献

参考文献12

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二级参考文献9

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共引文献3

同被引文献40

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引证文献4

二级引证文献8

中国医药工业杂志
2012年 第4期

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