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Polysubstituted tetrahydroquinolines were obtained in moderate to high yields (28% to 92%) and enantiomeric ratios (er 89:11 to 99:1) by a three‐component Povarov reaction using a chiral phosphoric acid catalyst. Significantly, post‐Povarov functional group interconversions allowed a rapid access to a library of 36 enantioenriched 4‐aminotetrahydroquinoline derivatives featuring five points of diversity...
Three cis‐selective Co(II)‐salen complexes have been developed for the asymmetric cyclopropanation of para‐fluorinated styrenes with ethyl diazoacetate. Increasing the steric reach of the C2‐symmetric ligand side chains improved the enantiomeric ratio of the reaction from 28:1 to 66:1. The methodology was exemplified by the gram‐scale synthesis of a lead compound for the treatment of castration‐resistant...
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