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Note | Regular issue | Vol 60, No. 6, 2003, pp.1425-1432
Published online, 14th April, 2003
DOI: 10.3987/COM-03-9753
Improved, Efficient Synthesis for Multigram-Scale Production of PSB-10, a Potent Antagonist at Human A3 Adenosine Receptors

Joachim Burbiel, Mark Thorand, and Christa E. Müller*

*Pharmaceutical Institute Poppelsdorf, University of Bonn, Kreuzbergweg 26, D-53115 Bonn, Germany

Abstract

The reported synthesis of PSB-10 (8-ethyl-4-methyl-2-(2,3,5-trichlorophenyl)-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]purin-5-one), a potent A3-selective adenosine receptor antagonist, gives only moderate yields and is not suitable for the production of PSB-10 on a multi-gram scale. Attempts to develop alternative routes and an improved procedure suitable for preparing large quantities of PSB-10, required for pharmacological studies, are described.