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Ring‐C bridged 1‐(pyrimidinyl)tetrahydrothebaines were convenience synthesized by a consecutive three‐component alkynylation–cyclocondensation sequence starting from 1‐ethynyl‐7α,8α‐(2,5‐dioxo‐N‐phenylpyrrolidino)‐[3,4‐h]‐6,14‐endo‐etheno‐tetrahydrothebaine, aroyl chlorides, and amidinium hydrochlorides. Several derivatizations and transformations of selected 1‐pyrimidinyl substituted tetrahydrothebaines were carried out. The analgesic activity of new type of hybrid compounds in the tail‐flick test in rats was evaluated. The data revealed that the antinociceptive potency was stroungly depended on the nature of the substituent in the C‐6 position of the pyrimidine nucleus. Docking study was undertaken to gain insight into the possible binding mode with the μ‐opioid receptor.

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