2-烷基-5(N,N-二取代胺甲基)-2-环戊烯酮类化合物的合成及其抗癌活性

The Synthesis and Anticancer Activities of 2-Alkyl-5-(N,N-disubstituted aminomethyl)-2-cyclopentenones

报道 2 庚基 5 (N ,N 二取代胺甲基 ) 2 环戊烯酮 (Ⅰ1)～ (Ⅰ4 )和 2 戊基 5 (N ,N 二取代胺甲基 ) 2 环戊烯酮 (Ⅱ1)～ (Ⅱ3 )的设计和合成 ,它们均属于 2 烷基 2 环戊烯酮 1的Mannich碱盐酸盐类化合物 .以环戊酮为起始原料 ,经Aldol缩合、双键转位和Mannich反应 ,合成了 7个目标化合物 ,其中 6个未见文献报道 ,其结构均经红外光谱、核磁共振氢谱和元素分析等数据证实 ,同时进行体外和体内抗癌活性筛选 .

A group of 2 alkyl 5 ( N,N disubstituted aminomethyl) 2 cyclopentenones(Ⅰ 1～Ⅰ 4,Ⅱ 1～Ⅱ 3)were designed and synthesized in the paper,which were Mannich base hydrochloride of 2 alkyl 2 cyclopentenones.They were synthesized from cyclopentanone via the Aldol condensation,transformation of the double bone position and the Mannich reaction.The chemical structures of the six novel chemical entities were characterized by IR, 1H NMR and EA.Preliminary in vitro and in vivo tests showed their potential anticancer activities.