【作者】 李继贞； 寇景平； 林英杰；

【Author】 Ji-Zhen Li, Jing-Ping Kou, Ying-Jie Lin* (College of Chemistry, Jilin University, 130012, Changchun)

【机构】 吉林大学化学学院；

【Abstract】 Heterocycles possessing guanidine skeletons have important biological activity, so their synthesis method draw chemistry worker’s sight and interest. We present here the novel synthesis method of cyclic guanidine 1-alkylsubstituted, 2-(N-alkylamino)-pyrimidin-4-ones from guanidine mediate. N-alkyl substituted nature β-amino acid reacted with thiourea substituted by pbfSO2 group to obtain the key compound guanidine 1, then the target six member heterocycles pyrimidin 2 were achieved via cyclization under TFA condition at room temperature. The total yield about 70%~75%.更多还原