Modification of 1-substituents in the 2-azabicyclo[2.1.1]hexane ring system; approaches to potential nicotinic acetylcholine receptor lingands from 2,4-methanoproline derivatives

The construction of novel derivatives has been made possible because of a nucleophilic substitution at a methylene attached to the bridgehead (1-) position of the 2-azabicyclo[2.1.1]hexane ring system. This provides access to epibatidine analogues, which contains heterocyclic substituents, and to homologation at the 1-position.