A Revised Modular Approach to (–)‐trans‐Δ8‐THC and Derivatives Through Late‐Stage Suzuki–Miyaura Cross‐Coupling Reactions

Abstract A revised modular approach to various synthetic (–)‐trans‐Δ8‐THC derivatives through late‐stage Suzuki–Miyaura cross‐coupling reactions is disclosed. Ten derivatives were synthesized allowing both sp2‐ and sp3‐hybridized cross‐coupling partners with minimal β‐hydride elimination. Importantly, we demonstrate that a para‐bromo‐substituted THC scaffold for Suzuki–Miyaura cross‐coupling reactions has been initially reported incorrectly in recent literature. Article type: Research Article Keywords: Tetrahydrocannabinol, Suzuki–Miyaura coupling, Cannabis derivatives, Cascade reactions, Heterocycles Authors: Victor R. L. J. Bloemendal ⚬, Daan Sondag, Hidde Elferink ⚬, Thomas J. Boltje