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[1]岳小龙,陈家浩,秦楠,等.抗糖尿病先导化合物Fla-CN的合成工艺研究[J].天津医科大学学报,2014,20(01):68-070.
　YUE Xiao-long,CHEN Jia-hao,QIN Nan,et al.Study on the synthesis process of anti-diabetic lead compound Fla-CN[J].Journal of Tianjin Medical University,2014,20(01):68-070.
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抗糖尿病先导化合物Fla-CN的合成工艺研究(PDF)
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《天津医科大学学报》[ISSN:1006-8147/CN:12-1259/R]

卷:
20卷
期数:
2014年01期
页码:
68-070
栏目:
技术与方法
出版日期:
2014-01-20

文章信息/Info

Title:
Study on the synthesis process of anti-diabetic lead compound Fla-CN
文章编号:
1006-8147(2014)01-0068-03
作者:
岳小龙; 陈家浩; 秦楠; 段宏泉
(天津医科大学药学院，天津市临床药物关键技术重点实验室，基础医学研究中心，天津300070)
Author(s):
 YUE Xiao-long;  CHEN Jia-hao;  QIN Nan;  DUAN Hong-quan
 （School of Pharmacy, Research Center of Basic Medical Sciences,Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, Tianjin Medical University, Tianjin 300070, China）
关键词:
抗糖尿病先导化合物; 黄酮衍生物Fla-CN; 合成工艺; 单因素考察
Keywords:
 ; anti-diabetes; flavonoid derivative Fla-CN; synthesis process; single-factor experiment
分类号:
R9
DOI:
-
文献标志码:
A
摘要:
 目的：对抗糖尿病先导化合物Fla-CN（3-O-[(E)-4-(4-氰基苯基)-3-烯-2-酮丁基]山萘酚）的合成工艺进行研究。方法：以对氰基苯甲醛和山奈酚为合成起始原料，先后经过Claisen-Schimidt反应，α, β-不饱和酮的α位溴代反应和醚化反应得到目标化合物Fla-CN，并从反应温度、底物浓度、反应物当量比以及催化剂等方面进行单因素考察试验，摸索最佳反应条件，建立合成工艺，提高反应总收率。结果：通过单因素考察等方法，建立了Fla-CN的合成工艺，目标产物的总收率显著提高，达到50%。结论：该工艺采用价廉易得的原料，简便的合成工艺与纯化手段，提高了反应收率，降低了生产成本。
Abstract:

 Objective: To explore the synthesis process of anti-diabetic lead compound Fla-CN (3-O-[(E)-4-(4-Cyanophenyl)-2-oxobut-3-en-1-yl]kaempferol). Methods: The target compound Fla-CN was prepared from 4-cyano benzaldehyde and kaempferol via Claisen-Schimidt condensation, α-bromination of theα, β-unsaturated ketone, and etherification reaction. To establish a suitable synthesis process for a high yield, we explored the preferred reaction conditions including reaction temperature, substrate concentration, reactants proportion and the catalyst by single-factor experiments. Results: The synthesis process of Fla-CN was established by single-factor experiments. The total yield had significantly increased to 50%. Conclusion: The preferred synthesis process could increase the total yield and reduce costs using cheap raw materials, convenient preparation and purification methods.


 

参考文献/References:

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备注/Memo

备注/Memo:

基金项目  国家自然科学基金面上项目（81373297）

作者简介  岳小龙（1988—），男，硕士在读，研究方向：天然产物结构改造；通信作者：段宏泉，E-mail：duanhq@tijmu.edu.cn。

更新日期/Last Update: 2014-03-28