Journal
SYNTHESIS-STUTTGART
Volume 50, Issue 2, Pages 211-226Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0036-1590938
Keywords
asymmetric synthesis; total synthesis; amino acids; chiral resolution; baclofen; synthetic methods; biocatalysis
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Funding
- Council of Scientific and Industrial Research, New Delhi
- Council of Scientific and Industrial Research, Ministry of Science and Technology, New Delhi [CSC-0108]
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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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