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Synfacts 2009(9): 0943-0943  
DOI: 10.1055/s-0029-1217615
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Norsertraline

Contributor(s): Philip Kocienski
L. K. Thalén, D. Zhao, J.-B. Sortais, J. Paetzold, C. Hoben, J. E. Bäckvall*
Stockholm University, Sweden
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Publication History

Publication Date:
21 August 2009 (online)

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Significance

Norsertraline is in clinical trials for the treatment of central nervous system disorders. The synthesis depicted uses Candida antarctica lipase B together with the racemization catalyst B in a one-pot dynamic kinetic resolution of primary amines. The lipase selectively acylates (S)-A whilst the remaining (R)-A is racemized by a catalyst derived in situ from B.