Synthesis of deuterium-labeled pregabalin

Authors


Liqin Chen, Hi-Tech Research Institute and State Key Laboratory of Materials-Oriented Chemical Engineering, Nanjing University of Technology, 5 Xinmofan Road, Nanjing, Jiangsu, 210009, China.

E-mail: liqin_chen@hotmail.com

Abstract

This paper describes the synthesis of deuterium-labeled pregabalin. The stable isotopic-labeled compound was obtained in nine steps starting from the commercially available 4-[2H11]methylvaleric acid as the stable-labeled reagent. It is used as an internal standard for analysis and metabolic studies.

Pregabalin labeled with 2H was obtained in nine steps using the commercially available 4-[2H11]methylvaleric acid as the stable-labeled reagent. The synthesis prevents deuterium from scrambling and offers the labeled compound with over 99% isotopic enrichment. Copyright © 2011 John Wiley & Sons, Ltd.

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