Synthesis and Anti-platelet Aggregation Activities of Novel Triazolo［4,5-d］pyrimidin Compounds
WANG Bing1,4, YANG Jing2, JIANG Xi-ming3, LIU Ying4, LIU Deng-ke4, WANG Ping-bao4
1. Graduate School, Tianjin Medical University, Tianjin 300070, China; 2. Department of Biology and Environmental Engineering, Tianjin Bohai Vocational and Technical College, Tianjin 300408, China; 3. Tianjin Pharmacn Medical Technology Co., Ltd., Tianjin 300384, China; 4. Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
Abstract：The aminopyrimidines(2) were obtained via the substitution reaction of 4,6-dichloro-2-(propylthio)pyrimidin-5-amine with primary amines. Diazotization and coupling reaction of 2 provided thiazoles(3). Twenty-six novel triazolo［4,5-d］pyrimidin compounds(6a~6z) were synthesized by the nucleophilic subsititution reaction of 3 with substituted amines and hydrolysis orderly. The structures were characterized by 1H NMR and ESI-MS. The anti-platelet aggregation activities were evaluated by platelet aggregation inhibition tests in rats. The results showed that 6a~6z exhibited certain anti-platelet aggregation activities. The inhibition rates of 6d, 6i and 6l were 61.9%, 69.3% and 71.2%, respectively.
王兵， 杨静， 姜希明， 刘颖， 刘登科， 王平保. 新型三唑并［4,5-d］嘧啶类化合物的合成及其抗血小板聚集活性[J]. 合成化学, 2016, 24(3): 185-191.
WANG Bing, YANG Jing, JIANG Xi-ming, LIU Ying, LIU Deng-ke, WANG Ping-bao. Synthesis and Anti-platelet Aggregation Activities of Novel Triazolo［4,5-d］pyrimidin Compounds. Chinese Journal of Synthetic Chemistry, 2016, 24(3): 185-191.
2016, Vol. 24 
