Myung Hee Jung

Synthesis and Muscarinic Activity of 1,2,3,4‐Tetrahydropyrimidine Derivatives

3‐Methyl‐1,2,3,4‐tetrahydropyrimidine‐5‐carbaldehyde O‐substituted oximes 4 and 1‐(3‐methyl‐1,2,3,4‐tetrahydropyrimidin‐5‐yl)ethanone O‐substituted oximes 9 have been prepared as bioisosteric congeners of arecoline which is a muscarinic agonist for treatment of Alzheimer s disease. Starting from pyrimidine‐5‐carbaldehyde 1, formation of the 3‐methylpyrimidinium salt and subsequent reduction afforded 1,2,3,4‐tetrahydropyrimidine derivatives which were converted into oxalate salts in the interest of purity and stability. Binding affinities of prepared compounds for the cloned human muscarinic M1 receptor (h‐M1) were determined by radioligand binding assay using [3H]‐N‐methylscopolamine (NMS).

Synthesis of quinolyl- and isoquinolyl heteroarylamines using palladium catalyzed suzuki cross-coupling reaction

Quinolyl- and isoquinolylboronic acids are prepared from 5-bromoquinoline and 5-bromoisoquinoline, respectively, via halogen-metal exchange. Suzuki cross-coupling of these compounds with haloheteroarylamine leading to thecorresponding heteroarylamine derivatives is described.