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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 study a new type of antitumor lead compound with high efficiency and low toxicity to drug-resistant tumors, N-substituted-4-piperidone and aromatic-formaldehyde derivatives were used as raw materials, respectively, with sodium hydroxide in ethanol or dry hydrogen chloride gas As catalyst, the aldol condensation reaction was carried out at 10 or 20 ℃ for 7 ~ 8 h and the progress of the reaction was monitored by TLC. Finally, three title compounds were synthesized by recrystallization and the yield was over 49%. 1HNMR, Its structure was characterized by crystal diffraction and melting point. The synthetic route has the advantages of mild reaction conditions and convenient operation, and the obtained derivative can be used for evaluating antitumor activity in the next experiment.