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合成3-(2-吡啶氨基)丙酸乙酯的工艺改进 被引量：3

Process Improvement on the Synthesis of Ethyl 3-(2-Pyridineamino) propanoate
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摘要 以2-氨基吡啶(2)和丙烯酸乙酯(3)为起始原料,经一步反应合成了凝血酶因子抑制剂达比加群酯的关键中间体3-(2-吡啶氨基)丙酸乙酯,其结构经1H NMR和ESI-MS确证。最佳反应条件为:2 120 mmol,n(2):n(3)=1.00:1.08,于100℃回流反应24 h,收率79.6%。 Ethyl 3-（2-pyridineamino）propanoate was synthesized by the reaction of 2-amino-pyridine with ethyl acrylate.The structure was confirmed by 1H NMR and ESI-MS.The optimum reaction conditions at 100 ℃ for 24 h were as follows：2 was 120 mmol,n（2）：n（3） was 1.00：1.08.The yield was 79.6% under the optimum reaction conditions.
作者 张伟光 蔡志强 刘洪强 徐为人 汤立达
机构地区 天津药物研究院天津市新药设计与发现重点实验室释药技术与药代动力学国家重点实验室 天津中医药大学 辽宁科技学院生物医药与化学工程学院
出处 《合成化学》 CAS CSCD 北大核心 2012年第6期782-783,786,共3页 Chinese Journal of Synthetic Chemistry
基金 国家重大新药创制专项基金资助项目(2011ZX09401-009)
关键词 2-氨基吡啶 3-(2-吡啶氨基)丙酸乙酯 药物合成 工艺改进 2-amino-pyridine 3-（2-pyridineamino）propanoate drug synthesis process improvement
分类号 O626.32 [理学—有机化学] R914.5 [医药卫生—药物化学]
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参考文献8

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二级参考文献12

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共引文献17

同被引文献22

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引证文献3

二级引证文献13

合成化学
2012年 第6期

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