4.5 Article

Enzymatic Method for the Synthesis of Blockbuster Drug Intermediates - Synthesis of Five-Membered Cyclic γ-Amino Acid and γ-Lactam Enantiomers

Journal

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
Volume 2008, Issue 31, Pages 5263-5268

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.200800723

Keywords

Amino acids; Enzyme catalysis; Lactams

Funding

  1. Hungarian Scientific Research Fund (OTKA) [K 71938, T 049407]

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A very efficient enzymatic method was developed for the synthesis of cyclic gamma-lactam and gamma-amino acid enantiomers, intermediates for drugs with a prominent turnover (e.g., abacavir and carbovir), through the CAL-B-catalysed enantioselective (E > 200) hydrolysis of the corresponding N-Boc protected and unprotected racemic gamma-lactams with H2O in iPr(2)O((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)

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