Biotechnology Letters

, Volume 18, Issue 8, pp 875–880

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

Authors

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

DOI: 10.1007/BF00154613

Cite this article as:
Black, T.D., Briggs, B.S., Evans, R. et al. Biotechnol Lett (1996) 18: 875. doi:10.1007/BF00154613

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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Copyright information

© Chapman & Hall 1996