Scheme 1. Synthesis of Reactive Agonist Ligands (3a−c) for Acyl Transfer to the A2AAR.
Reagents and yields: a. acyl anhydride, pyridine, 30-40%; b. EDC·HCl, DMF, 60%; c. RCO2H, DCC, DMAP, DMF, 30-50%, for 3b and 3c. d. PyBOP/DIEA, DMF, 70%, for 3a.
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