Asymmetric synthetic strategies of (R)-(–)-baclofen: an antispastic drug
P Ramesh, D Suman, KSN Reddy - Synthesis, 2018 - thieme-connect.com
P Ramesh, D Suman, KSN Reddy
Synthesis, 2018•thieme-connect.comBaclofen is an antispastic drug used as a muscle relaxant in the treatment of the paroxysmal
pain of trigeminal neuralgia, spasticity of the spinal cord and cerebral origin. Baclofen
resides biological activity exclusively in its (R)-(–)-enantiomer. In this review, various
asymmetric synthetic strategies for (R)-(–)-baclofen are described. 1 Introduction 2
Resolution Synthetic Approaches 2.1 Chemical Resolution 2.2 Biocatalytic Resolution 3
Asymmetric Desymmetrization 3.1 Catalytic Enantioselective Desymmetrization 3.2 …
pain of trigeminal neuralgia, spasticity of the spinal cord and cerebral origin. Baclofen
resides biological activity exclusively in its (R)-(–)-enantiomer. In this review, various
asymmetric synthetic strategies for (R)-(–)-baclofen are described. 1 Introduction 2
Resolution Synthetic Approaches 2.1 Chemical Resolution 2.2 Biocatalytic Resolution 3
Asymmetric Desymmetrization 3.1 Catalytic Enantioselective Desymmetrization 3.2 …
Baclofen is an antispastic drug used as a muscle relaxant in the treatment of the paroxysmal pain of trigeminal neuralgia, spasticity of the spinal cord and cerebral origin. Baclofen resides biological activity exclusively in its (R)-(–)-enantiomer. In this review, various asymmetric synthetic strategies for (R)-(–)-baclofen are described.
1 Introduction
2 Resolution Synthetic Approaches
2.1 Chemical Resolution
2.2 Biocatalytic Resolution
3 Asymmetric Desymmetrization
3.1 Catalytic Enantioselective Desymmetrization
3.2 Enzymatic Desymmetrization
4 Chiral Auxiliary Induced Asymmetric Synthesis
4.1 Asymmetric Michael Addition
4.2 Asymmetric Aldol Addition
4.3 Asymmetric Nucleophilic Substitution
5 Asymmetric Reduction
5.1 Catalytic Asymmetric Hydrogenation
5.2 Bioreduction
6 Catalytic Asymmetric Conjugate Addition
7 Conclusion
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