A high-throughput screening protocol for fast evaluation of enantioselective catalysts.

A new high-throughput screening protocol that allows fast evaluation of enantioselective catalysts has been developed. The usefulness of norephedrine-derived beta-amino alcohols as catalysts for the enantioselective alkylation of prochiral aldehydes has been determined by simultaneous screening of three representative substrates. GC analysis of the crude product mixture using a selectively modified cyclodextrin as the chiral stationary phase avoids time-consuming workup procedures. The chemical yield, enantioselectivity, substrate specificity, and catalytic activity of the chiral catalysts as well as the induced absolute configuration have been determined in a single screening experiment and two short GC runs.