Abstract

AbstractA 16‐member library of C2‐symmetric modular chiral BINOL‐oxazoline Schiff base copper(II) complex catalysts generated in situ was easily generated in a one‐pot, three‐component manner. This approach avoided the need for isolation and characterization of ligands and greatly improved the catalyst screening efficiency. This modular catalyst library was evaluated in the asymmetric Henry reaction, for which good yields (up to 98 %) and good to excellent enantioselectivities (up to 98 % ee) were obtained under mild conditions.

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