Abstract
AbstractWe rationally designed and successfully developed novel dipeptidic proline amide–isothiouronium catalysts for asymmetric conjugate addition reactions between various aldehydes and nitroolefins, which generated 1,4‐addition products with up to 95% yields, 92:8 syn‐diastereoselectivity, and 96% enantiomeric excess. The catalysts, which were prepared via simple methylation of the corresponding thiourea, can provide the desired enantiomeric syn‐1,4‐adducts by exchanging the configuration of the N‐terminal proline moiety.
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