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微波促进合成抗肿瘤化合物Combretastatin A-4
引用本文:刁银军,罗小会,卢政明,肖珊美.微波促进合成抗肿瘤化合物Combretastatin A-4[J].广东化工,2012,39(7):60-60,59.
作者姓名:刁银军  罗小会  卢政明  肖珊美
作者单位:金华职业技术学院,浙江金华,321007
基金项目:浙江省中医药科学研究基金计划(2011ZB156):浙江省教育厅科研计划项目
摘    要:目的:微波催化脱羧合成抗肿瘤药物Combretastatin A-4。方法:以3,4,5-三甲氧基苯乙酸为起始原料合与异香草醛经Perkin反应缩合、微波催化脱羧反应合成Combretastatin A-4。结果:合成产物经核磁共振氢谱、碳谱、质谱、熔点等确证其化学结构,总收率均达到40%左右。结论:微波催化脱羧合成Combretastatin A-4反应产率高,反应条件简便,立体选择性高,反应时间短,环境友好。

关 键 词:微波促进  抗肿瘤化合物  Combretastatin  A-4  立体选择法

Microwave Promote to Synthesis Anticancer Agent Combretastatin A-4
Diao Yinjun,Luo Xiaohui,Lu Zhengming,Xiao Shanmei.Microwave Promote to Synthesis Anticancer Agent Combretastatin A-4[J].Guangdong Chemical Industry,2012,39(7):60-60,59.
Authors:Diao Yinjun  Luo Xiaohui  Lu Zhengming  Xiao Shanmei
Affiliation:(Jinhua PolyTec, Jinhua 321007, China)
Abstract:Purpose: To synthesize the anticancer agent Combretastatin A-4 via microwave promotion decarboxylation reactions. Method: 3,4,5-Trimethoxyphenylacetic acid and isovanilline were used as starting materials to prepare combretastatin A-4 through Perkin reaction and decarboxylation reactions. Result: The structures of target compounds were confirmed by IH-NMR, 13C-NMR, MS and Melting point; the overall yields were about 40 %. Conclusion: Combretastatin A-4 is synthesized in very good yields through microwave irradiation. The synthetic routes developed herein require simple reaction conditions, and yield high stereo-selectivity of cis-confbrmation and eco-friendly.
Keywords:microwave promotion  anticanceragent: combretastatinA-4: stereo-selectivity
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