Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists

A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A(2A) antagonists is described. SAR studies led to compound 14 with excellent potency ( K-i = 0.4 nM), selectivity ( A(1)/A(2A) > 100), and efficacy ( MED 10 mg/ kg po) in the rat haloperidol- induced catalepsy model for Parkinson's disease. (C) 2008 Elsevier Ltd. All rights reserved.