Abstract: AimTo design and synthesize new chiral 8-(substituted)amino-analogues of 3-［(tetrahydro-2-furanyl)methyl］ benzomorphans, to expand knowledge of the structure-activity relationship(SAR) for 8-aminobenzomorphan.MethodsTarget compounds were synthesized from the 8- triflate of the optically active 3-［(tetrahydro-2-furanyl)methyl］-2,6-methano- benzomorphans using Pd-catalyzed aminations.Opioid receptor binding experiments were performed to evaluate their biological activities.ResultsBoth 8-amino and 8-phenylamino analogues showed lower binding affinity for μ, δ and κ receptors than corresponding 8-hydroxy-3-［(tetrahydro-2-furanyl)methyl］-2,6-methano-benzomorphan in vitro. ConclusionThe relative poor binding affinity of the target compounds did not warrant conducting the in vivo studies to determine if they have the profile(κ agonist/μ antagonist) that will be potentially useful in the treatment of drug addiction.Further study is in progress.