(À)-Cytisine (1) has occupied a pivotal role in nicotinic pharmacology as a partial agonist at the α4β2 subtype of neuronal nicotinic acetylcholine receptor (nAChR).[1] More recently because of this partial agonist profile, cytisine provided the discovery lead for varenicline (2), Pfizer s smoking cessation agent which was launched in 2006.[2, 3] Recent interest in the chemistry of cytisine (1) has been high because of a lack of understanding as to the ...