2－（N－芳胺甲基）－5－（E）戊亚基环戊酮衍生物的合成及其抗炎活性研究

Synthesis of 2-(N-arylaminomethyl)-5-(E) Pentylidene Cyclopentanoe Derivatives and Studies on Their Antiinflammatory Activity

报道了２－（Ｎ－芳胺甲基）－５－（Ｅ）戊亚基环戊酮（Ⅰ）和与其互为双健位置异构体的２－（Ｎ－芳胺甲基）－５－戊基环戊－２－烯酮（Ⅱ）的设计和合成。两系列均属２－Ｎ－芳胺Ｍａｎｎｉｃｈ碱环戊酮衍生物。以环戊酮为起始原料，分别经２－（Ｎ－二甲胺基甲基）－５－（Ｅ）戊亚基环戊酮（Ａ）和２－（Ｎ－二甲胺基甲基）－５－戊基环戊－２－烯酮（Ｂ），合成了１３个未见文献报道的目标化合物。探讨了Ｍａｎｎｉｃｈ碱与取代芳胺进行胺交换反应的活性。对所合成的部分目标化合物进行了抗炎活性的药理筛选。

The design and synthesis of the compound 2-(N-arylamino methyl)-5-(E) pentylidene cyclopentanone(Ⅰ) and its structural isomer of double bond 2-(N-aryl amino methyl)-5-pentyl-2-cyclopenten-1-one(Ⅱ) are recounted in this paper. These two series of compounds are all derivaturies of 2-N-aryl amino Mannich base. Through both 2-(N-dimethylaminomethyl)-5- (E) pentylidene cyclopentanone(A) and 2-(N-dimethylaminomethyl) -5-pentyl-2-cyclopenten-1-one(B), all the 13 targeting compounds have been synthesized from cyclopentanone and all of the compounds have not been found in literature. Besides, the amino exchange reaction of the Mannich base with the substituted toomatic amines has been investigated. Partially targeting compounds have been examined input their antiinflammatory activity.