Synthesis of (1-azabicyclo[3.3.0] octanyl)methyl-substituted aromatic heterocycles and their muscarinic activity

Abstract

In our development of drugs 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 describe 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.