1-取代哌啶-4-酮芳甲酰腙的合成及其抗白血病活性

Synthesis and Anti-leukemia Activity of 1-Substituted Piperidin-4-one Arylformylhydrazones

以取代苄胺或伯胺为原料,依次经过Michael加成、Dieckmann缩合、水解脱羧、酰腙化反应合成了10个未见文献报道的1-取代哌啶-4-酮芳甲酰腙9a～9j,化合物结构经1H NMR,IR,MS和元素分析确证.初步的生物活性测试表明,部分化合物能有效抑制白血病K562细胞的增殖,具有潜在的抗白血病活性.

Ten novel 1-substituted piperidin-4-one arylformylhydrazones 9a～9j were synthesized with substituted benzylamines or primary amines as raw materials via a series of Michael addition,Dieckmann condensation,hydrolytic decarboxylation reactions and hydrazone formation reactions.Their structures were elucidated and confirmed by 1H NMR,IR,MS techniques and elemental analysis.The preliminary biologic activity tests indicate that some of the target compounds have good antiproliferative activities against K562 cells and have potential anti-leukemia bioactivity.