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Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives
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Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives
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| Han, Jianlin; Escorihuela Fuentes, Jorge; Fustero Lardiés, Santos; Landa, Aitor; Soloshonok, Vadim A.; Sorochinsky, Alexander | |||
| Aquest document és un/a article, creat/da en: 2022 | |||
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| 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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