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An asymmetric synthesis to the dendrobatid alkaloid (−)-epibatidine has been described, featuring chiral resolution of both optically pure 7-azabicyclo[2.2.1]heptanecarboxylic acid, and subsequent transformations to (−)-epibatidine. The methodology provides a flexible access to various substituted chiral epibatidine analogues.

Graphical abstract: Synthesis of (−)-epibatidine

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