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2000
Volume 22, Issue 7
  • ISSN: 1570-1786
  • E-ISSN: 1875-6255

Abstract

Brivaracetam is a relatively new racetam drug for the treatment of epilepsy, synthesis of which with proper stereocontrol remains challenging. Herein we describe a solvent-free lactamization method for the development of two efficient synthetic routes to brivaracetam. The key method is a one-step condensation of amines with chiral α-carboxyethyl-β-propyl butyrolactone under neat conditions that proceed through tandem decarboxylation and lactamization. The lactam obtained using benzylamine was converted to ()-3-propyl pyrrolidinone, a key intermediate to brivaracetam. Whereas, the lactam obtained from the condensation of ()-2-amino butanol was further transformed into brivaracetam.

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2025-09-08

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Synthesis of Epilepsy Drug Brivaracetam through Solvent-free Lactamization
Lett. Org. Chem. 22, 567 (2025); https://doi.org/10.2174/0115701786350134241220173948
/content/journals/loc/10.2174/0115701786350134241220173948
/content/journals/loc/10.2174/0115701786350134241220173948
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  • Article Type:     Research Article
Keyword(s): Brivaracetam; debenzylation; PIDA-TEMPO oxidation; solvent-free; tandem reaction; γ-lactam

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