| (2R,4R)-4-甲基-2-哌啶甲酸乙酯的合成工艺改进 |
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| 引用本文： | 张磊,张灿.(2R,4R)-4-甲基-2-哌啶甲酸乙酯的合成工艺改进[J].中南药学,2012,10(8):588-590. |
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| 作者姓名： | 张磊 张灿 |
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| 作者单位： | 中国药科大学新药研究中心,南京,211198 |
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| 摘 要： | 目的 优化(2R,4R)-4-甲基-2-哌啶甲酸乙酯的合成工艺.方法 以S-(-)-α-甲基苄胺为原料,与乙醛酸乙酯反应得到(S)-1-苯乙基亚胺基]乙酸乙酯,与异戊二烯进行环合后,再经不对称氢化和脱保护反应制得(2R,4R)-4-甲基-2-哌啶甲酸乙酯.结果 总收率从17.0％提高至47.6％.结论 本工艺可有效地降低生产成本.
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| 关 键 词： | (2R 4R)-4-甲基-2-哌啶甲酸乙酯 阿加曲班 凝血酶抑制剂 合成 |
Synthesis of ethyl(2R,4R)-4-methylpiperidine-2-carboxylate |
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| ZHANG Lei
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ZHANG Can.Synthesis of ethyl(2R,4R)-4-methylpiperidine-2-carboxylate[J].Central South Pharmacy,2012,10(8):588-590. |
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| Authors: | ZHANG Lei ZHANG Can |
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| Institution: | *(Center of Drug Discovery,China Pharmaceutical University,Nanjing 211198) |
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| Abstract: | Objective To optimize the synthesis of ethyl(2R,4R)-4-methylpi-peridine-2-carboxylate.Methods Ethyl(2R,4R)-4-methylpiperidine-2-carboxylate was synthesized from(S)-1-phenylethanamine and ethyl 2-oxoacetate to obtain ethyl (S)-1-phenylethylimino]acetate,which underwent cyclization with isoprene followed by asymmetric hydrogenation and deprotection.Results The overall yield was improved from 17.0% to 47.6%.Conclusion This method is effective for reducing production costs. |
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| Keywords: | ethyl(2R 4R)-4-methylpiperidine-2-carboxylate argatroban thrombin inhibitor synthesis |
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