作者:Serge Djekou、Armand Gellis、Patrice Vanelle、Hussein El-Kashef
DOI:10.1002/jhet.5570430513
日期:2006.9
[3,2-a]pyrimidin-5-one (2) is obtained by cyclocondensation of 2-aminothiazole with ethyl 4-chloroacetoacetate. This product was shown to react with various nitronate or malonate anions under microwave irradiation to give potentially bioactive 6-nitro-5H-thiazolo[3,2-a]pyrimidin-5-ones. Extension to other anions centered on S atom allows for the generalization this synthetic procedure.
通过2-氨基噻唑与4-氯乙酰乙酸乙酯的环缩合反应,得到7-氯甲基-6-硝基-5 H-噻唑并[3,2 - a ]嘧啶-5-酮(2)。该产物显示在微波辐射下与各种硝酸根或丙二酸根阴离子反应,可产生具有生物活性的6-硝基-5 H-噻唑并[3,2 - a ]嘧啶-5-酮。扩展到以S原子为中心的其他阴离子可以推广这种合成方法。