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Synthesis of novel pyrrolidin-2-ones: γ-aminobutyric acid cyclic analogues

✍ Scribed by S. Al Akoum Ebrik; B. Rigo; C. Vaccher; M-P. Vaccher; N. Flouquet; M. Debaert; P. Berthelot

Publisher
Journal of Heterocyclic Chemistry
Year
1998
Tongue
English
Weight
355 KB
Volume
35
Category
Article
ISSN
0022-152X

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✦ Synopsis

Abstract

Some new N‐substituted pyrrolidin‐2‐ones, cyclic analogues of baclofen and of 3‐(5‐methoxybenzo‐[b]furan‐2‐yl)‐γ‐aminobutyric acid, have been prepared and characterized, starting from 4‐(4‐chlorophenyl)‐pyrrolidin‐2‐one and 4‐(5‐methoxybenzo[b]furan‐2‐yl)pyrrolidin‐2‐one.

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✍ Roger G. Hall; Peter D. Kane; Helmut Bittiger; Wolfgang Froestl 📂 Article 📅 1995 🏛 John Wiley and Sons 🌐 French ⚖ 252 KB

## Abstract The synthesis of a new radioligand, which binds with high selectivity and affinity (K~D~ = 7.4 nM) to the GABA‐B receptor, is described. A Wittig‐Horner approach was employed to prepare an unsaturated protected intermediate (6), suitable for tritiation and deprotection.