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).
CITATION STYLE
Black, T. D., Briggs, B. S., Evans, R., Muth, W. L., Vangala, S., & Zmijewski, M. J. (1996). o-phthalyl amidase in the synthesis of Loracarbef: Process development using this novel biocatalyst. Biotechnology Letters, 18(8), 875–880. https://doi.org/10.1007/BF00154613
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