A comprehensive review of pharmacological and medical aspects of the muscar
inic class of acetylcholine agonists and antagonists is presented. The ther
apeutic benefits of achieving receptor subtype selectivity are outlined and
applications in the treatment of Alzheimer's disease are discussed. A sele
ction of chemical routes are described, which illustrate contemporary metho
dology for the synthesis of chiral medicinal compounds (asymmetric synthesi
s, chiral pool, enzymes). Routes to bicyclic intrannular amines and intramo
lecular Diels-Alder reactions are highlighted.