Synthesis and Evaluation of a Series of Heterobiarylamides That Are Centrally Penetrant Metabotropic Glutamate Receptor 4 (mGluR4) Positive Allosteric Modulators (PAMs)
作者:Darren W. Engers、Colleen M. Niswender、C. David Weaver、Satyawan Jadhav、Usha N. Menon、Rocio Zamorano、P. Jeffrey Conn、Craig W. Lindsley、Corey R. Hopkins
DOI:10.1021/jm9005065
日期:2009.7.23
We report the synthesis and evaluation of a series or heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.
Solid-supported Pt-catalyzed remote C-H etherification of arylamines: A simple and practical approach for the synthesis of aromatic ethers
A simple and practical approach for a direct remote C-H etherification of arylamines with alcohol is developed herein by using a solid-supported Pt catalyst, hence providing a valuable method for the synthesis of aromatic ethers. The catalyst can easily be recovered from the reaction mixture and reused for six times without apparent loss of activity. Control experiments suggest that a radical pathway