Enzymatic method for the synthesis of blockbuster drug intermediates - Synthesis of five-membered cyclic γ-amino acid and γ-lactam enantiomers

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Abstract

A very efficient enzymatic method was developed for the synthesis of cyclic γ-lactam and γ-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 γ-lactams with H2O in iPr2O.

Original languageEnglish
Pages (from-to)5263-5268
Number of pages6
JournalEuropean Journal of Organic Chemistry
Issue number31
DOIs
Publication statusPublished - Nov 1 2008

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Keywords

  • Amino acids
  • Enzyme catalysis
  • Lactams

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry

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