Microwave-Assisted Synthesis of 4-Substituted 2-Methylthiopyrimidines

被引:5
作者
Thomann, Andreas [1 ]
Boerger, Carsten [2 ]
Empting, Martin [1 ]
Hartmann, Rolf W. [1 ,3 ]
机构
[1] Univ Saarland, Helmholtz Inst Pharmaceut Res Saarland, D-66123 Saarbrucken, Germany
[2] Univ Saarland, PharmBioTec GmbH, D-66123 Saarbrucken, Germany
[3] Univ Saarland, D-66123 Saarbrucken, Germany
关键词
green chemistry; pyrimidine; combinatorial chemistry; medicinal chemistry; nucleophilic aromatic substitution; BIOLOGICAL EVALUATION; DERIVATIVES; ROUTES;
D O I
10.1055/s-0033-1340860
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Typically, SNAr reactions at 4-chloro-2-methylthiopyrimidine are carried out employing DMF and sodium hydride under inert gas as well as prolonged reaction times. Herein, we describe a mild and rapid microwave-assisted synthesis to achieve 4-substituted 2-methylthiopyrimidnes from the corresponding chlorine precursor. Moderate to excellent yields were obtained in a green chemistry fashion requiring only few minutes of reaction time.
引用
收藏
页码:935 / 938
页数:4
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