Abstract:
Neuronal nicotinic acetylcholine receptors of the a7 subtype are potential targets for drug development in the treatment of Alzheimer’s disease. The Delphinium alkaloid methyllycaconitine is a potent and selective a7 sub-type selective nicotinic acetylcholine receptor antagonist. The total synthesis of this pharmacologically active alkaloid has not yet been achieved. A summary of semisynthetic methods to prepare methyllycaconitine is presented. Existing synthetic strategies used to prepare E, AE, AEF, ABE, ABDE, ABEF ring analogues of methyllycaconitine are reviewed for the first time.