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Investigators at AstraZeneca Detail Findings in Nitrogenous Group Transferases

February 18, 2014

By a News Reporter-Staff News Editor at Life Science Weekly -- Researchers detail new data in Enzymes and Coenzymes. According to news reporting from Cheshire, United Kingdom, by NewsRx journalists, research stated, "Screening of 60 transaminases using three different amine donors found that the omega-transaminase from Vibrio fluvialis together with (S)-alpha-methylbenzylamine to be the most promising combination to deliver the desired (S)-1-(5-fluoropyrimidin-2-yl)-ethylamine (2) in almost quantitative conversion. The process was further improved by the addition of immiscible organic solvents with toluene identified as most suitable concerning the distribution of the reactants without negatively impacting the performance of the biocatalyst."

The news correspondents obtained a quote from the research from AstraZeneca, "Further process optimization using commercial enzyme preparations of V. fluvialis led to product/catalyst ratios of 15 g/g cell dry weight. This approach led to a process that provided (S)-1-(5-fluoropyrimidin-2-yl)ethylamine (2) in 77% yield with 99.8% ee. In addition, a recombinant E. coli-based whole-cell biocatalyst was also designed and applied to this process. The use of this low cost enzyme formulation gave product of similar quality to that obtained using the commercial formulation of V. fluvialis. This process was further optimized and scaled-up to deliver (S)-1-(5-fluoropyrimidin-2-yl)ethylamine (2)with a yield of 66% and an optical purity of 97.3% ee."

According to the news reporters, the research concluded: "These results confirm the efficiency and competitiveness of the transaminase technology for the production of chiral amines."

For more information on this research see: Efficient Synthesis of (S)-1-(5-Fluoropyrimidin-2-yl)ethylamine Using an omega-Transaminase Biocatalyst in a Two-Phase System. Organic Process Research & Development, 2013;17(9):1117-1122. Organic Process Research & Development can be contacted at: Amer Chemical Soc, 1155 16TH St, NW, Washington, DC 20036, USA. (American Chemical Society -; Organic Process Research & Development -

Our news journalists report that additional information may be obtained by contacting R.E. Meadows, AstraZeneca, Pharmaceut Dev, Macclesfield SK10 2NA, Cheshire, United Kingdom. Additional authors for this research include K.R. Mulholland, M. Schurmann, M. Golden, H. Kierkels, E. Meulenbroeks, D. Mink, O. May, C. Squire, H. Straatman and A.S. Wells (see also Enzymes and Coenzymes).

Keywords for this news article include: Europe, Cheshire, Ethylamines, Transaminases, United Kingdom, Enzymes and Coenzymes, Nitrogenous Group Transferases

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Source: Life Science Weekly

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