Article
Syntheses and biological properties of cysteine-reactive epibatidine derivatives.
Bioorganic & medicinal chemistry letters - 24 Mar 2003
Che Christian, Petit Grégory, Kotzyba-Hibert Florence, Bertrand Sonia, Bertrand Daniel, Grutter Thomas, Goeldner Maurice
Abstract excerpt
The synthesis of epibatidine derivatives modified at the 2-position of the pyridine or pyrimidine rings by reactive functions are described for potential irreversible site-directed coupling reactions on cysteine mutants of neuronal nicotinic acetylcholine receptors. An improved synthesis of the 7-azabicyclo[2,2,1]hepta-2,5-diene key intermediate has been developed to allow reproducible syntheses of the...
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