Organocatalyzed Deracemization of Δ2‐Pyrrolin‐4‐ones

Abstract Racemic pyrrolin‐4‐ones, accessible from α ‐amino acids, undergo asymmetric stereoselective organocatalyzed 1,4‐additions to trans ‐β‐nitrostyrenes (up to 98 % ee ; dr up to 97:3). From a series of typical organocatalysts, the best performance was achieved using (+)‐camphor‐1,3‐diamine‐derived bifunctional organocatalysts. A broad substrate scope and some follow‐up modifications have been demonstrated. magnified image