Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives.
Jianlin HanJorge EscorihuelaSantos FusteroAitor LandaVadim A SoloshonokAlexander SorochinskyPublished in: Molecules (Basel, Switzerland) (2022)
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.
Keyphrases
- molecular docking
- structure activity relationship
- systematic review
- working memory
- neuropathic pain
- electronic health record
- big data
- molecular dynamics simulations
- solid state
- spinal cord
- machine learning
- skeletal muscle
- adipose tissue
- blood brain barrier
- high resolution
- cerebral ischemia
- weight loss
- brain injury
- drug induced
- electron transfer
- simultaneous determination