Synthesis of (1-Azabicyclo[3.3.0]octanyl)methyl-Substituted Aromatic Heterocycles and Their Muscarinic Activity

In our development of srugs effective against Alzheimer's disease, we have researched a series of aromatic compounds having a characteristic cyclic amine, 1-azabicyclo[3.3.0]octane ring.In this report, we descride synthesis of a series of aromatic heterocycles with the 1-azabicyclo[3.3.0]octane ring and their pharmacological evaluation. 3-Amino-5-(1-azabicyclo[3.3.0]octan-5-yl)methyl-1, 2, 4-oxadiazole(2b) showed the highest M1 selectivity.