Economical synthesis of tert-butyl (S)-3-aminopyrrolidine-1-carboxylate from L-aspartic acid

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

Keywords:

• Aminopyrrolidine derivatives
• aspartic acid
• phase transfer catalyst

Disclosure statement

The authors confirm that this article content has no conflict of interest.

Additional information

Funding

We are grateful to the National Natural Science Foundation of China (No. 81670594) and Cuiying Scientific and Technological Innovation Program of Lanzhou University Second Hospital (No. CY2017-MS05) for the financial support.