By a News Reporter-Staff News Editor at Life Science Weekly -- New research on General Chemical Research is the subject of a report. According to news reporting originating from York, United Kingdom, by NewsRx correspondents, research stated, "The development of cost-effective and sustainable catalytic methods for the production of enantiomerically pure chiral amines is a key challenge facing the pharmaceutical and fine chemical industries. This challenge is highlighted by the estimate that 40-45% of drug candidates contain a chiral amine, fueling a demand for broadly applicable synthetic methods that deliver target structures in high yield and enantiomeric excess."
Our news editors obtained a quote from the research from the University of York, "Herein we describe the development and application of a 'toolbox' of monoamine oxidase variants from Aspergillus niger (MAO-N) which display remarkable substrate scope and tolerance for sterically demanding motifs, including a new variant, which exhibits high activity and enantioselectivity toward substrates containing the aminodiphenylmethane (benzhydrylamine) template. By combining rational structure-guided engineering with high-throughput screening, it has been possible to expand the substrate scope of MAO-N to accommodate amine substrates containing bulky aryl substituents. These engineered MAO-N biocatalysts have been applied in deracemization reactions for the efficient asymmetric synthesis of the generic active pharmaceutical ingredients Solifenacin and Levocetirizine as well as the natural products ®-coniine, ®-eleagnine, and ®-leptaflorine."
According to the news editors, the research concluded: "We also report a novel MAO-N mediated asymmetric oxidative Pictet-Spengler approach to the synthesis of ®-harmicine."
For more information on this research see: Engineering an Enantioselective Amine Oxidase for the Synthesis of Pharmaceutical Building Blocks and Alkaloid Natural Products. Journal of the American Chemical Society, 2013;135(29):10863-10869. Journal of the American Chemical Society can be contacted at: Amer Chemical Soc, 1155 16TH St, NW, Washington, DC 20036, USA. (American Chemical Society - www.acs.org; Journal of the American Chemical Society - www.pubs.acs.org/journal/jacsat)
The news editors report that additional information may be obtained by contacting D. Ghislieri, University of York, Dept. of Chem, Struct Biol Lab, York YO10 5YW, N Yorkshire, United Kingdom. Additional authors for this research include A.P. Green, M. Pontini, S.C. Willies, I. Rowles, A. Frank, G. Grogan and N.J. Turner (see also General Chemical Research).
Keywords for this news article include: York, Europe, Oxidase, Engineering, United Kingdom, Enzymes and Coenzymes, General Chemical Research
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