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.