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Herein, we developed an electronic effect‐guided rational design strategy to enhance the enantioselectivity of Candida antarctica lipase B (CALB) mutants towards bulky pyridyl(phenyl)methanols. Compared to W104A mutant previously reported with reversed S‐stereoselectivity toward sec‐alcohols, three mutants (W104C, W104S and W104T) displayed significant improvement of S‐enantioselectivity in the kinetic...
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