抗糖尿病先导化合物Fla-CN的合成工艺研究  

Study on the synthesis process of anti-diabetic lead compound Fla-CN

作　　者：岳小龙[1] 陈家浩[1] 秦楠[1] 段宏泉[1] 

机构地区：[1]天津医科大学药学院基础医学研究中心,天津市临床药物关键技术重点实验室,天津300070

出　　处：《天津医科大学学报》2014年第1期68-70,F0003,共4页Journal of Tianjin Medical University

基　　金：国家自然科学基金面上项目(81373297)

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萘酚为合成起始原料,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。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-eyano benzaldehyde and kaempferol via Claisen- Schimidt condensation, a-bromination of the a, β-unsaturated ketone, and etherification reaction. To establish a suitable synthesis process for a high yield. The preferred reaction conditions including reaction temperature, substrate concentration, reactants proportion and the catalyst were explored by single-factor experiments. Results： The synthesis process of Fla-CN was established by single-factor experiments. The total yield hacl 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.

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 

分 类 号：R9[医药卫生—药学]