Caffeic acid phenethyl ester and its benzoyl derivatives:synthesis and X-ray structural analysis

咖啡酸苯乙酯及其苯甲酰基衍生物:合成和单晶X衍射分析(英文)

Caffeic acid phenethyl ester （CAPE）, the main biologically active component of propolis, has been successfully synthesized from caffeic acid and β-bromoethylbenzene catalyzed by Na2CO3 in a mixed solvent of HMPA-CH3CN. To better understand the struc^re-activity relationship of CAPE, phenylethyl-monobenzoylcinnamate and phenylethyl-dibenzoylcinnamate were prepared. Meanwhile, the structure of phenylethyl-monobenzoylcinnamate was confirmed by single-crystal X-ray diffiaction.

在Na2CO3的催化下,咖啡酸和β溴乙基苯在非质子性混合溶剂HMPACH3CN中高收率地合成天然蜂胶中主要的生物活性成分咖啡酸苯乙酯(CAPE)。为了更好地探究CAPE的构效关系和活性机理,我们首次成功地合成了单、双苯甲酰基取代的咖啡酸苯乙酯产物,同时单苯甲酰基取代产物结构通过单晶X衍射被确定。