3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity
2-Methyl-6-(phenylethynyl)pyridine (3), a potent noncompetitive mGlu5 receptor antagonist widely used to characterize the pharmacology of mGlu5 receptors, suffers from a number of shortcomings as a therapeutic agent, including off-target activity and poor
Cosford, Nicholas D. P.,Tehrani, Lida,Roppe, Jeffrey,Schweiger, Edwin,Smith, Nicholas D.,Anderson, Jeffrey,Bristow, Linda,Brodkin, Jesse,Jiang, Xiaohui,McDonald, Ian,Rao, Sara,Washburn, Mark,Varney, Mark A.
Palladium-Catalyzed Reactions of Terminal Acetylenes and Olefins with Halo-1,3-azoles
The palladium-catalyzed reactions of 4-bromo- and 5-bromothiazoles, as well as 4-bromo and 5-bromooxazoles with terminal acetylenes gave ethynyl derivatives in 43-89percent yields, whereas the reactions of 2-bromothiazoles and iodo-N-methylimidazoles affo