| 4-(N-叔丁氧羰基)氨甲基-1-(N-叔丁氧羰基)吡咯烷-3-醇的合成 |
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| 引用本文： | 刘巧云,谢婷,陈文华. 4-(N-叔丁氧羰基)氨甲基-1-(N-叔丁氧羰基)吡咯烷-3-醇的合成[J]. 安徽农业科学, 2012, 40(3): 1481-1482 |
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| 作者姓名： | 刘巧云 谢婷 陈文华 |
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| 作者单位： | 常州工程职业技术学院,江苏省应用酶工程技术研究开发中心,江苏常州213164 |
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| 基金项目： | 常州工程职业技术学院科研基金立项课题 |
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| 摘 要： | [目的]改进4-(N-叔丁氧羰基)氨甲基-1-(N-叔丁氧羰基)吡咯烷-3-醇的合成工艺。[方法]以4-氰基-1-(N-叔丁氧羰基)吡咯烷-3-酮为原料,经硼氢化钠、漆原钴催化加氢还原、氨基保护"一锅法"制得目标化合物。[结果]改进的工艺采用漆原钴催化加氢代替原来的氢化铝锂还原,总收率由原来的75%提高至88%,结构经1HNMR确证。[结论]该工艺操作安全,适用于工业化生产。
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| 关 键 词： | 4-(N-叔丁氧羰基)氨甲基-1-(N-叔丁氧羰基)吡咯烷-3-醇 硼氢化钠 漆原钴 合成 |
The Synthesis of 4- (N-t-butoxycarbony) aminomethyl -1- (N-t-butoxycarbony) pyrrolidin -3-alcohol |
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| Affiliation: | LIU Qiao-yun et al(Applied Enzyme Engineering Technology R&D Center of Jiangsu,Changzhou Institute of Engineering Technology,Changzhou,Jiangsu 213164) |
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| Abstract: | [Objective] To improve the synthesis technology of 4-(N-t-butoxycarbony)aminomethyl-1-(N-t-butoxycarbony)pyrrolidin-3-alcohol.[Method] 4-(N-t-butoxycarbony)aminomethyl-1-(N-t-butoxycarbony)pyrrolidin-3-alcohol was synthesized starting from 4-cyano-1-(N-t-butoxycarbony)pyrrolidin-3-ketone by one-pot of reduction with NaBH4,hydrogenation reduction in the presence of Urushibara-Co and amino protection with Boc.[Result] Experiment results showed the total yield increased from 75% to 88% by reduction of Urushibara-Co instead of LiAlH4 in the improved reduction reaction.Structure of the product was confirmed by 1HNMR.[Conclusion] The synthesis technology is suitable for industrialization with operation safety. |
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| Keywords: | 4-(N-t-butoxycarbony)aminomethyl-1-(N-t-butoxycarbony)pyrrolidin-3-alcohol NaBH4 Urushibara-Co |
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