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Keywords:

  • deuterium;
  • labeled;
  • synthesis;
  • pregabalin

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.