- A straightforward entry to 7-azabicyclo[2.2.1]heptane-l-carbonitriles in the synthesis of novel epibatidine analogues
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This paper presents the synthesis of epibatidine analogues by a straightforward one-pot method for the synthesis of 7azabicyclo[2.2.1]heptane-1- carbonitriles, starting from cyclohexanones bearing a leaving group at the 4-position. In situ imine formation
- Heugebaert, Thomas,Van Hevele, Joke,Couck, Wouter,Bruggeman, Vicky,Van Jeught, Sarah Der,Masschelein, Kurt,Stevens, Christian V.
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supporting information; experimental part
p. 1017 - 1020
(2010/04/25)
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- STRAIGHTFORWARD ENTRY TO 7-AZABICYCLO[2.2.1]HEPTANE-1-CARBONITRILES AND SUBSEQUENT SYNTHESIS OF EPIBATIDINE ANALOGUES
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The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
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Page/Page column 9
(2009/12/02)
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