2-对甲氧基苯亚甲基-5-取代氨甲基环戊酮衍生物的合成

2-对甲氧基苯亚甲基-5-取代氨甲基环戊酮衍生物的合成

康影, 李玉兰, 徐颍, 计志忠

1. 沈阳药科大学药学系药化教研室, 沈阳 110015;
2. 沈阳药科大学合成药物研究室, 沈阳 110015

收稿日期:1996-07-17 修回日期:1996-12-24 出版日期:1997-09-15 发布日期:1997-09-15

Synthesis and Antiinflammatory Activity of 2-(4-Methoxy benzylidene)-5-aminomethyl Cyclopentanone Derivatives

Ying Kang, Yu-Lan Li, Ying Xu, Zhi-Zhong Ji

1. Department of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110015; 
2. Laboratory of Synthetic Drugs, Shenyang Pharmaceutical University, Shenyang 110015

Received:1996-07-17 Revised:1996-12-24 Online:1997-09-15 Published:1997-09-15

摘要/Abstract

摘要： 本文设计合成了10个未见文献报道的2-对甲氧基苯亚甲基-5-取代胺甲基环戊酮衍生物, 均经红外光谱、核磁共振谱及元素分析, 证实其化学结构。采用角叉菜胶诱发的大鼠足爪肿胀模型进行抗炎活性的初步筛选。在化学合成中还证实: Mannich碱的胺交换反应是消除加成反应。

关键词: 环戊酮衍生物, 抗炎活性, 胺交换反应

Abstract: In this paper, ten new derivatives of 2-(4-methoxybenzylidene)-5-aminomethyl cyclopentanone were designed and synthesized. The structures of all these ten title compounds have been confirmed by IR, ¹H NMR and elemental analysis. The compounds have been examined for the anti-inflammatory activity on carrageenin-induced rat paw edema test. Through chemical synthesis, we have confirmed that the amino exchange reaction proceeds by an elimination-addition mechanism.

Key words: Cyclopentanones, Antiinflammatory activity, Amino-exchange reaction

Supporting: ^*Project supported by the National Natural Science Foundation of China.

康影, 李玉兰, 徐颍, 计志忠. 2-对甲氧基苯亚甲基-5-取代氨甲基环戊酮衍生物的合成[J]. .

Ying Kang, Yu-Lan Li, Ying Xu, Zhi-Zhong Ji. Synthesis and Antiinflammatory Activity of 2-(4-Methoxy benzylidene)-5-aminomethyl Cyclopentanone Derivatives[J]. .

[1]	孔秋云, 杭楠, 张超, 李树春, 李中军, 孙洋, 孟祥豹. 作用于炎症小体的α,β-不饱和酮类化合物的合成及活性评价[J]. 中国药学(英文版), 2018, 27(5): 295-306.
[2]	全东琴, 崔光华, 董华进, 阮金秀. 醋酸地塞米松静注乳剂的抗炎活性及动物组织分布研究[J]. , 2001, 10(2): 90-93.
[3]	曹丽, 罗崇念, 卞庆亚, 肖培根. 小檗胺抗炎活性的实验研究[J]. , 1999, 8(2): 93-94.
[4]	董金华, 徐莉英, 秦华, 许丁元, 李莉, 计志忠. 2-(E)-(3-甲氧基-4-羟基苯亚甲基)-5-(N-取代胺甲基) 环戊酮的合成及其抗炎活性研究[J]. , 1998, 7(4): 186-190.