Download PDF
Synthesis 1985; 1985(12): 1100-1104
DOI: 10.1055/s-1985-31439
paper
© Georg Thieme Verlag, Rüdigerstr. 14, 70469 Stuttgart, Germany. All rights reserved. This journal, including all individual contributions and illustrations published therein, is legally protected by copyright for the duration of the copyright period. Any use, exploitation or commercialization outside the narrow limits set by copyright legislation, without the publisher's consent, is illegal and liable to criminal prosecution. This applies in particular to photostat reproduction, copying, cyclostyling, mimeographing or duplication of any kind, translating, preparation of microfilms, and electronic data processing and storage.

Synthesis of N-Substituted Muscimol Derivatives Including N-Glycylmuscimol

Michael Frey* , Volker Jäger
  • *Institut für Organische Chemie der Universität, Am Hubland, D-8700 Würzburg, Federal Republic of Germany
Further Information

Publication History

Publication Date:
27 September 2002 (online)

 PDF Download  Permissions and Reprints All articles of this category

The preparation of museimol (a potent but toxic GABA neurotransmitter agonist), from dimethyl acetylenedicarboxylate via methyl 3-hydroxyisoxazole-5-carboxylate and the corresponding amide, has been improved and extended to a general synthesis of N-alkyl and N,N-dialkyl derivatives. The efficient route to muscimol itself [muscimol itself costs 60 -170 DM/10 mg] has enabled a study of its chemistry to be undertaken, a first result of which is its incorporation into a peptide, i.e. the preparation of N-glycylmuscimol.