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Synthesis 2024; 56(04): 549-552
DOI: 10.1055/s-0042-1751470
DOI: 10.1055/s-0042-1751470
special topic
Synthetic Development of Key Intermediates and Active Pharmaceutical Ingredients (APIs)
An Alternative Formal Synthesis of (S)-(+)-Vigabatrin
Abstract
An improved synthesis of chirally pure advanced pyrrolidone intermediate of the (S)-(+)-vigabatrin, an antiseizure active pharmaceutical ingredient (API) is reported. The synthesis is developed using commercially available, cheaper amino acid (R)-methionine. Meldrum’s acid served as a two-carbon homologation unit to access the pyrrolidone intermediate in a short synthetic sequence. The sequence to pyrrolidone intermediate is scalable and eludes the use of organometallic pyrophoric reagents on a large scale.
Supporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0042-1751470.
- Supporting Information
Publikationsverlauf
Eingereicht: 17. März 2023
Angenommen nach Revision: 07. Juni 2023
Artikel online veröffentlicht:
03. Juli 2023
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