3-乙酰基香豆素衍生物的合成及抗血小板聚集活性  

Synthesis and Anti-platelet Aggregation Activity of 3-Acety-coumarins Derivatives

作　　者：何冰 刘红 肖维玉 张强 张群英 HE Bing;LIU Hong;XIAO Wei-yu;ZHANG Qiang;ZHANG Qun-ying(College of Pharmacy,Anhui University of Chinese Medicine,Hefei 230038,China)

机构地区：[1]安徽中医药大学药学院,安徽合肥230038

出　　处：《化学试剂》2020年第11期1305-1308,共4页Chemical Reagents

摘　　要：以水杨醛、乙酰乙酸乙酯为原料合成3-乙酰基香豆素,其酮羰基与盐酸羟胺反应得到肟,利用肟羟基与不同碳数的二溴烷烃反应得到相应的溴代肟醚,再与吗啉反应得到5个标题化合物。其结构经过红外光谱、核磁共振氢谱和质谱确证。采用Born比浊法,对中间体和5个标题化合物进行了以二磷酸腺苷(ADP)为诱导剂的体外抗血小板聚集的活性试验,结果表明,标题化合物的活性均强于对照药阿司匹林,其中3-乙酰香豆素肟的活性最强。3-Acetyl-coumarin was obtained by the reactions between salicylaldehyde and ethyl acetoacetate,whose keto carbonyl group was then treated with hydroxylamine hydrochloride to afford 3-acetyl-coumarin oxime.3-Acetyl-coumarin oxime treated with dibromoalkanes(2~6 carbons) in the presence of K2CO3 to provide the compounds 3-acethlcoumarin bromoether.These compounds were then reacted with morpholine to obtain five target compounds.Structures were confirmed by 1HNMR,IR and MS.The intermediate and five target compounds were tested for the anti-platelet aggregation activity of ADP as an inducer by Born turbidimetry.In vitro-platelet aggregation activity results showed the title compounds showed significant anti-platelet aggregation activities comparable to stronger than that of control aspirin.Particularly,3-acetyl-coumarin oxime showed excellent anti-platelet aggregation activity.

关 键 词：水杨醛 盐酸羟胺 3-乙酰基香豆素 肟醚 抗血小板凝聚 

分 类 号：R916[医药卫生—药学]