Evaluates stereoselective synthesis in octahydrobenzoisoquinolines, suggesting a new approach for δ-opioid receptor agonists.
An amide-based polyene cyclization has been developed for the stereoselective synthesis of octahydrobenzo[f]isoquinolines. This reaction employs E-olefins as substrates and features a wide substrate scope, affording products in good yields with high diastereoselectivity. Notably, the stereochemical outcome is precisely controlled by the reaction temperature, representing a novel activation mode in polyene chemistry. Importantly, the synthesized octahydrobenzo[f]isoquinolines exhibit selective agonism for the δ-opioid receptor, providing valuable insights for developing more effective δ-opioid receptor agonists.
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Cao et al. (2026) studied this question.
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