广东化工
廣東化工
엄동화공
GUANGDONG CHEMICAL INDUSTRY
2012年
7期
60-60,59
,共2页
刁银军%罗小会%卢政明%肖珊美
刁銀軍%囉小會%盧政明%肖珊美
조은군%라소회%로정명%초산미
微波促进%抗肿瘤化合物:Combretastatin%A-4:立体选择法
微波促進%抗腫瘤化閤物:Combretastatin%A-4:立體選擇法
미파촉진%항종류화합물:Combretastatin%A-4:입체선택법
microwave promotion%anticanceragent: combretastatinA-4: stereo-selectivity
目的:微波催化脱羧合成抗肿瘤药物CombretastatinA-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CombretastatinA-4。结果:合成产物经核磁共振氢谱、碳潜、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CombretastatinA-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。
目的:微波催化脫羧閤成抗腫瘤藥物CombretastatinA-4。方法:以3,4,5-三甲氧基苯乙痠為起始原料閤與異香草醛經Perkin反應縮閤、微波催化脫羧反應閤成CombretastatinA-4。結果:閤成產物經覈磁共振氫譜、碳潛、質譜、鎔點等確證其化學結構,總收率均達到40%左右。結論:微波催化脫羧閤成CombretastatinA-4反應產率高.反應條件簡便,立體選擇性高,反應時間短,環境友好。
목적:미파최화탈최합성항종류약물CombretastatinA-4。방법:이3,4,5-삼갑양기분을산위기시원료합여이향초철경Perkin반응축합、미파최화탈최반응합성CombretastatinA-4。결과:합성산물경핵자공진경보、탄잠、질보、용점등학증기화학결구,총수솔균체도40%좌우。결론:미파최화탈최합성CombretastatinA-4반응산솔고.반응조건간편,입체선택성고,반응시간단,배경우호。
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.