N-取代-3,5-二芳亚甲基-4-哌啶酮衍生物的合成与表征  

Synthesis and characterization of N-substituted-3,5-bis(arylidene)-4-piperidone derivatives

作　　者：孙居锋[1] 李珂珂[1] 于晨[1] 代现平[1] 

机构地区：[1]滨州医学院药学院,山东烟台264003

出　　处：《化学试剂》2011年第7期613-616,共4页Chemical Reagents

基　　金：国家自然科学基金资助项目(30970298)

摘　　要：为了研究一类高效低毒对耐药肿瘤有效的新型抗肿瘤先导化合物,以N-取代-4-哌啶酮和芳甲醛衍生物为原料,分别以氢氧化钠的乙醇溶液或干燥的氯化氢气体作催化剂,在10或20℃经过7～8 h的羟醛缩合反应,TLC监测反应进程,最后经重结晶合成了3种标题化合物,收率达49%以上,并采用1HNMR、X-射线单晶衍射结合熔点对其结构进行了表征。该合成路线反应条件温和、操作简便,所得衍生物可用于下一步实验中抗肿瘤活性评价。In order to research a kind of high potency,low toxicity potential antitumour leading compounds,a few N-substituted-3,5-bis（arylidene）-4-piperidones were synthesized taking N-substituted-4-piperidones and formaldehyde derivatives as starting materials with alcoholic NaOH or dry hydrogen chloride as catalyst by aldol condensation reaction inspected by TLC on the condition of 10 ℃ or 20 ℃,7～8 h,followed by recrystalization.The yield is over 49%.The structures were characterized by 1HNMR,X-ray crystallography with melting points.It was a convenient and efficient method in high yield.The compounds are used for antitumour evaluation in our next work.

关 键 词：芳甲醛衍生物 羟醛缩合反应 4-哌啶酮衍生物 新型抗肿瘤先导化合物 

分 类 号：O626.32[理学—有机化学]