Biotechnology Letters

, Volume 18, Issue 8, pp 875–880 | Cite as

o-Phthalyl amidase in the synthesis of loracarbef: Process development using this novel biocatalyst

  • Thomas D. Black
  • Barbara S. Briggs
  • Robert Evans
  • William L. Muth
  • Surya Vangala
  • Milton J. Zmijewski
Article

Summary

A dephthalylation step utilizing a novel enzyme, o-phthalyl amidase, was developed. This step was part of a potentially new large scale synthetic route for a novel beta-lactam antibiotic Loracarbef. The enzyme was isolated from the organism Xanthobacter agilis. Purification of the enzyme to near homogeneity was accomplished by a 3-step procedure. Studies indicated that the phthalimido group can be opened chemically to generate the o-phthalyl derivative. This enzyme then can remove the phthalyl group from o-phthalylated amides. Optimization of the process was achieved by combining these two hydrolysis steps. Conversion yields of 85–97.8% (mol/mol) were obtained from reactions at substrate concentrations of 5–10% (w/v).

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References

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Copyright information

© Chapman & Hall 1996

Authors and Affiliations

  • Thomas D. Black
    • 1
  • Barbara S. Briggs
    • 1
  • Robert Evans
    • 1
  • William L. Muth
    • 1
  • Surya Vangala
    • 1
  • Milton J. Zmijewski
    • 1
  1. 1.Lilly Research Laboratories, Process Research and DevelopmentIndianapolisUSA

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