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Updated: Jun 22, 2026

Enzymatic Cascade Reactions for the Synthesis of Chiral Amino Alcohols from L-lysine
Published on: February 16, 2018
Chemoenzymatic synthesis of rivastigmine based on lipase-catalyzed processes
Juan Mangas-Sánchez1, María Rodríguez-Mata, Eduardo Busto
1Departamento de Química Orgánica e Inorganica, Instituto Universitario de Biotecnología de Asturias, Universidad de Oviedo, c/ Julián Claveria s/n, Oviedo 33071, Spain.
Abstract:
A straightforward chemoenzymatic synthesis of enantiomerically pure rivastigmine has been efficiently carried out under mild reaction conditions, with Candida antarctica lipase B responsible for the stereoselective acetylation of the corresponding (R)-alcohol or amine. An exhaustive enzymatic study has been developed exploring the possibilities of carry out enzyme recycling, scaling up the enzymatic process and development of a dynamic kinetic resolution procedure for the production of adequate enantiomerically pure precursors of rivastigmine. Total chemoenzymatic synthesis of this pharmaceutical has been performed in good overall yield from commercially available 3-methoxyacetophenone.
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