Novel and highly effective chemoenzymatic synthesis of (2<Emphasis Type="Italic">R</Emphasis>)-2-[4-(4-cyano-2-fluorophenoxy)phenoxy]butylpropanoate based on lipase mediated transesterification |
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Authors: | Genlin Zhu Risheng Yao Huixia Zhu Huai Wang |
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Institution: | (1) Department of Pharmaceutical Engineering, School of Medical Engineering, Hefei University of Technology, Hefei, 230009, Anhui, P. R. China |
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Abstract: | (2R)-2-4-(4-Cyano-2-fluorophenoxy)phenoxy]butylpropanoate (cyhalofop-butyl, CyB) was synthesized by a chemoenzymatic route involving
enantioselective transesterification with Candida antarctica lipase B (Novozym 435). The optimum organic solvent, acyl donor, a
w
, reaction temperature and shaking rate for the transesterification were acetonitrile, n-butanol, 0.11, 45°C and 200 rpm, respectively. Under the optimum conditions, the maximum substrate conversion and the enantiomeric
purity of the product were 96.9 and >99%, respectively. The total yield and enantiomeric purity of CyB by this chemoenzymatic
synthesis were 60.4 and >99%, respectively; 15.3 and 21% higher than that of the traditional way (45 and 78%). |
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