Concise Synthesis of the Antidepressive Drug Candidate GSK1360707 by a Highly Enantioselective Gold-Catalyzed Enyne Cycloisomerization Reaction

Out of depression: Indeed, no depressing results are obtained from a gold-catalyzed enyne cycloisomerization controlled by phosphoramidite ligands with TADDOL-related but acyclic backbones (see scheme; Cbz=benzyloxycarbonyl). The “triple-reuptake inhibitor” GSK1360707 was obtained in excellent yield and optical purity, therefore highlighting the relevance of asymmetric gold catalysis for practical applications