Position: Home > Articles > The Synthesis of 4-(N-t-butoxycarbony)aminomethyl-1-(N-t-butoxycarbony)pyrrolidin-3-alcohol
Journal of Anhui Agricultural Sciences
2012,40
(3)
1481-1482
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
作 者：
刘巧云;谢婷;陈文华
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
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
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。
译 名：
The Synthesis of 4-(N-t-butoxycarbony)aminomethyl-1-(N-t-butoxycarbony)pyrrolidin-3-alcohol
作 者：
LIU Qiao-yun et al(Applied Enzyme Engineering Technology R&D Center of Jiangsu,Changzhou Institute of Engineering Technology,Changzhou,Jiangsu 213164)
关键词：
4-(N-t-butoxycarbony)aminomethyl-1-(N-t-butoxycarbony)pyrrolidin-3-alcohol;NaBH4;Urushibara-Co
摘 要：
[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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