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

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

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