Asymmetric synthesis of irnigaine was achieved starting from an enantiopure β amino ester 5 using the condensation of amino alcohol 2 with acetylacetone and the subsequent intramolecular cyclization as the key steps. Asymmetric synthesis of irnigaine was achieved starting from an enantiopure β amino ester 5 using the condensation of amino alcohol 2 with acetylacetone and the subsequent intramolecular cyclization as the key steps.