Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives

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Date
2022
Author
Han, Jianlin ORCID
Escorihuela, Jorge
Fustero, Santos ORCID
Landa Alvarez, Aitor
Soloshonok, Vadym Anatolievch ORCID
Sorochinsky, Alexander ORCID
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Molecules 27(12) : (2022) // Article ID 3797
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http://hdl.handle.net/10810/57260
Abstract
γ-Aminobutyric acid (GABA) represents one of the most prolific structural units widely used in the design of modern pharmaceuticals. For example, β-substituted GABA derivatives are found in numerous neurological drugs, such as baclofen, phenibut, tolibut, pregabalin, phenylpiracetam, brivaracetam, and rolipram, to mention just a few. In this review, we critically discuss the literature data reported on the preparation of substituted GABA derivatives using the Michael addition reaction as a key synthetic transformation. Special attention is paid to asymmetric methods featuring synthetically useful stereochemical outcomes and operational simplicity.
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© 2022 by the authors.Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https:// creativecommons.org/licenses/by/ 4.0/).
Except where otherwise noted, this item's license is described as © 2022 by the authors.Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https:// creativecommons.org/licenses/by/ 4.0/).