1166916-61-5Relevant articles and documents
Chemoenzymatic synthesis of rivastigmine based on lipase-catalyzed processes
Mangas-Sanchez, Juan,Rodriguez-Mata, Maria,Busto, Eduardo,Gotor-Fernandez, Vicente,Gotor, Vicente
, p. 5304 - 5310 (2009)
(Chemical Equation Presented) 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.