Journal of Organic Chemistry 2010-05-07

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

Kiwon Han, Cheolwoo Kim, Jaiwook Park, Mahn-Joo Kim

Index: J. Org. Chem. 75(9) , 3105-8, (2010)

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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.