The first asymmetric synthesis of (+)-abresoline has been achieved starting from the (S)-1-(aryl)homoallylic amine, which was prepared anantioselectively by the method based on allylation of the (R)-2'-(2-naphthyl)-bearing hydroxyoxime ether. This synthetic route employs the TiCl4-induced intramolecular Mannich-type cyclization of the 1-azadiene-bearing ketal amine as the key steps to afford stereoselectively the cis-2,6-disubstituted piperidine, followed by CBr4/PPh3-induced dehydrocyclization for the elaboration of the amino alcohol to the trans-4-arylquinolizidine. (c) 2005 Elsevier Ltd. All rights reserved.