Improved, efficient synthesis for multigram-scale production of PSB-10, a potent antagonist at human A3 adenosine receptors

被引:0
|
作者
Burbiel, J [1 ]
Thorand, M [1 ]
Müller, CE [1 ]
机构
[1] Univ Bonn, Inst Pharmazeut, D-53115 Bonn, Germany
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中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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 A(3)-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.
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页码:1425 / 1432
页数:8
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