6533b82efe1ef96bd1293222
RESEARCH PRODUCT
Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives
Jianlin HanJorge EscorihuelaSantos FusteroAitor LandaVadim A. SoloshonokAlexander Sorochinskysubject
Baclofenasymmetric Michael additionγ-aminobutyric-acid derivativesOrganic ChemistryPregabalinPharmaceutical ScienceStereoisomerismQuímica farmacèuticapharmaceuticalsneurological drugsAnalytical ChemistryReaccions químiqueschiral auxiliariesChemistry (miscellaneous)Drug DiscoveryMolecular Medicineenantioselective organocatalysisPhysical and Theoretical Chemistrygamma-Aminobutyric AcidMedicamentsdescription
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. This research was funded by the National Natural Science Foundation of China (No. 21761132021), and IKERBASQUE, Basque Foundation for Science. The financial support from the University of the Basque Country UPV/EHU (UFIQOSYC11/22), Basque Government (GVgrant IT1236-19), and Ministerio de Ciencia e Innovación (grant PID2019-109633GBC21) for. A.L. are also acknowledged.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2022-01-01 |