14 beta-(2-bromoacetamido)morphine and 14 beta-(2-bromoacetamido)morphinone.

摘要: 14 beta-(2-Bromoacetamido)morphine (6) and beta-(2-bromoacetamido)morphinone (9) were prepared preferably from the adduct of thebaine 1-chloro-1-nitrosocyclohexane, which on reduction in methanol solution gave 14-aminocodeinone (2) corresponding ketal (3). When tested a receptor-binding assay, IC50 values 6 9 15 10 nM, respectively. If incubation time during assay was increased to 30 min, irreversible binding both ligands observed.