Small Peptide‐Catalyzed Enantioselective Addition of Ketones to Nitroolefins

The direct small peptide‐catalyzed enantioselective Michael addition of ketones to nitroolefins is presented. Simple di‐ and tripeptides derived from alanine catalyze the asymmetric Michael additions with high stereoselectivity and furnish the corresponding Michael products in high yield with up to 68 : 1 dr and 98% ee. The study demonstrates that small, readily prepared peptides with increased structural complexity as compared to the parent amino acid mediate the asymmetric Michael reaction with superior reactivity and enantioselectivity.