Abstract
AbstractThe first catalytic enantioselective direct aldol reaction of 3‐acetylcoumarins to pyrazole‐4,5‐diones is reported and shown to proceed through noncovalent substrate activation by a quinine‐derived bifunctional tertiary amino‐amide as the catalyst. The densely functionalized products, consisting of an oxygen‐containing quaternary stereocenter and bearing two biologically relevant heterocycles, are generally obtained in high yields with moderate to excellent enantioselectivities.
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