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Synthesis and Biological Evaluation of (±)-Epibatidine and the Congeners
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1994
Year
Inhibitory ActivityMedicinal ChemistryBioorganic ChemistryBiochemistryNatural SciencesMedicineHydroxy FunctionTotal SynthesisBiological EvaluationNon-opiate Antinociceptive AlkaloidPharmacologyPharmaceutical ChemistrySynthetic ChemistryEnantioselective SynthesisDrug DiscoveryNatural Product Synthesis
A total synthesis of the non-opiate antinociceptive alkaloid (±)-epibatidine and its congeners is described, in which the key step is the reductive elimination of hydroxy function in 8a. The hydrogenolysis of 8a proceeded smoothly with retention of the configuration to afford 9a. Biological evaluation of these compounds is also included.