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Synfacts 2010(8): 0853-0853  
DOI: 10.1055/s-0030-1257746
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of (S)-Rivastigmine

Contributor(s): Philip Kocienski
K. Han, C. Kim, J. Park*, M.-J. Kim*
Pohang University of Science and Technology, Korea
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Publication History

Publication Date:
22 July 2010 (online)

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Significance

Rivastigmine (Exelon®) is an acetylcholinesterase inhibitor that is prescribed for the treatment of mild to moderate dementia in patients with Alzheimer’s disease and Parkinson’s disease. The key step in the synthesis depicted is a dynamic kinetic resolution of the benzylic secondary alcohol B involving a lipase (Novozyme 435) coupled with a polymer-bound racemization catalyst (C).