| Title | Chemoenzymatic Synthesis of Rivastigmine Based on Lipase-Catalyzed Processes. | | Author(s) | Mangas-Sánchez J, Rodríguez-Mata M, Busto E, Gotor-Fernández V, Gotor V | | Institution | Departamento de Quimica Organica e Inorganica, Instituto Universitario de Biotecnologia de Asturias, Universidad de Oviedo, c/ Julian Claveria s/n, Oviedo 33071, Spain. | | Source | J Org Chem 2009 Jun 25. | | 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. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19555095 |
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