No abstract

Efficient Synthesis of AMP579, a Novel Adenosine A1/A2 Receptor Agonist.-A highly regioselective route to title adenosine agonist (X) is presented, involving the condensation of an alkylsulfonamide (II) with a pyridine synthon (III) as key step. The sulfonamide protecting group then effectively prevents undesired cyclization pathway during formation of the deazapurine ring (IX). Title compound (X) is obtained in 35% overall yield in 8 steps starting from amino alcohol (I). -(SLEDESKI, ADAM W.; KUBIAK, GREGORY G.; O'BRIEN, MICHAEL K.; POWERS, MATTHEW R.; POWNER, TORY H.; TRUESDALE, LARRY K.; J. Org. Chem. 65 (2000) 23, 8114-8118; Process Chem., Rhone-Poulenc Rorer, Collegeville, PA 19426, USA; EN)