Chemoenzymatic Synthesis of Rivastigmine via Dynamic Kinetic Resolution as a Key Step

Pohang University of Science and Technology, Geijitsu, Gyeongsangbuk-do, South Korea
The Journal of Organic Chemistry (Impact Factor: 4.72). 03/2010; 75(9):3105-8. DOI: 10.1021/jo9027374
Source: PubMed


A practical and efficient procedure for the synthesis of rivastigmine was developed. This procedure includes dynamic kinetic resolution using a polymer-bound ruthenium complex and a lipase in combination as a key step. Enantiopure (-)-rivastigmine was obtained from commercially available 3'-hydroxyacetophenone via five steps in overall 57% yield.

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Available from: Kiwon Han, Jan 07, 2014
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