The Synthesis of 9-(1-Azetidinyl)-1,2,3,4-tetrahydroacridine

Abstract

tX&&&i -Synthesis of analogue (2) of tacrine is described in which the primary amino group is replaced by the azetidine moiety.The synthesis was accomplished in two steps from the acridinone derivative 10.This involved conversion of 1 0 to triflate 11, followed by treatment with azetidine to give the target compound 2.The recent success of 9-amino-l,2,3.4-tetrahydroacridine(tacrine) (1) in the treatment of Alzheimer's disease has inspired our interest in the synthesis of certain related