Process for the preparation of epibatidine

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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546 15, 546338, 546335, 546337, C07D40104

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active

055457410

ABSTRACT:
The invention relates to a process for the preparation of racemic or optically active epibatidine of the Formula XIV ##STR1## which comprises subjecting racemic or optically active epi-epibatidine-of the Formula XIII ##STR2## to epimerization in the presence base. The advantage of the process is that readily available starting materials are used and the procedure is suitable for industrial scale productions too.
Epibatidine is a known highly affective analgesic active ingredient.

REFERENCES:
patent: 4245112 (1981-01-01), Ficini et al.
patent: 4503053 (1985-03-01), Nedelec et al.
patent: 4845126 (1989-07-01), Hidasi et al.
patent: 5296494 (1994-03-01), Lavielle et al.
Fletcher et al. J. Org. Chem, 1994, 59, pp. 1771-1778.

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