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Z. Naturforsch. 2012,
67b, 1123 – 1126
doi:10.5560/ZNB.2012-0127
Efficient Enzymatic Amine Resolution at High Substrate Input Using Diethyl Malonate as an Acyl Donor of Low Hazard Potential
1 Department of Chemistry and Pharmacy, University of Erlangen-Nürnberg, Henkestr. 42, 91054 Erlangen, Germany
2 Evonik Industries AG, Health & Nutrition, Rodenbacher Chaussee 4, 63457 Hanau-Wolfgang, Germany
3 Current address: Faculty of Chemistry, Bielefeld University, Universitätsstr. 25, 33615 Bielefeld, Germany
Reprint requests to Prof. Dr. Harald Gröger. Fax: +49 521 1066146. E-mail:
harald.groeger@uni-bielefeld.de
Received May 17, 2012 / published online October 8, 2012
Dedicated to Professor Dr. Dr. Heribert Offermanns on the occasion of his 75th birthday
Diethyl malonate turned out to be both a “green” and highly efficient acyl donor in the lipase-catalyzed resolution of amines, thus representing an attractive alternative to currently applied acyl donors. By means of this acyl donor a highly efficient enzymatic process for the resolution of amines, running at high substrate input of up to 200 g/L in an organic solvent classified as “usable” according to the Pfizer Solvent Selection Guide, is presented.
Key words: Amines, Amides, Enantioselective Synthesis, Biocatalysis, Enzymatic Resolution