Chemoenzymatic synthesis of rivastigmine via dynamic kinetic resolution as a key step.

Department of Chemistry and Bionanotechnology Center, Pohang University of Science and Technology, San-31 Hyojadong, Pohang 790-784, Korea.
The Journal of Organic Chemistry (Impact Factor: 4.56). 03/2010; 75(9):3105-8. DOI: 10.1021/jo9027374
Source: PubMed

ABSTRACT 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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