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Economical synthesis of tert-butyl (S)-3-aminopyrrolidine-1-carboxylate from L-aspartic acid
Synthetic Communications ( IF 1.8 ) Pub Date : 2018-09-17 , DOI: 10.1080/00397911.2018.1509093
Zhi-Jian Han 1 , Yang-Bing Li 1 , Bao-Hong Gu 2 , Yu-Min Li 2 , Hao Chen 1, 2
Affiliation  

Abstract 3-Aminopyrrolidine building block was used as the intermediate for many pharmaceutically active substances. Starting from L-aspartic acid, optically active (S)-tert-butyl-3-aminopyrrolidine-1-carboxylate was synthesized, and the reaction conditions were optimized in each step. The procedure of each step was discussed in detail and could be useful for the industrial preparation. This process was featured by readily available starting material, mild reaction conditions, easy work-up, and economy. Graphical Abstract

中文翻译:

由L-天冬氨酸经济合成(S)-3-氨基吡咯烷-1-羧酸叔丁酯

摘要 3-氨基吡咯烷结构单元被用作许多药物活性物质的中间体。以L-天冬氨酸为原料,合成了具有旋光性的(S)-叔丁基-3-氨基吡咯烷-1-羧酸酯,并在各步骤中优化了反应条件。详细讨论了每一步的程序,可用于工业制备。该工艺具有原料易得、反应条件温和、后处理容易、经济等特点。图形概要
更新日期:2018-09-17
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