Facile Synthesis and Evaluation of Cell A549 Growth Inhibitory Activity of 4-Aryl-6-aryloxymethylmorpholin-3-one Derivatives  

作　　者：谭伟 赵宝祥 石梅 沙磊 苗俊英 申东守 

机构地区：[1]Institute of Organic Chemistry, School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China [2]Institute of Developmental Biology, School of Life Science, Shandong University, Jinan, Shandong 250100, China [3]Department of Chemistry and Research Institute of Natural Sciences, Changwon National University, Changwon, GN, 641-773, South Korea

出　　处：《Chinese Journal of Chemistry》2006年第3期396-400,共5页中国化学（英文版）

摘　　要：A series of 4-aryl-6-aryloxymethylmorpholin-3-one derivatives were synthesized very efficiently from readily available starting compounds in two steps. Ring opening reactions of epoxides with aniline compounds on alumina gave corresponding β-aminoalcohols （3）. The resulting β-aminoalcohols were reacted with 2-chloroacetyl chloride to yield the desired 4-aryl-6-aryloxymethylmorpholin-3-one derivatives （5）. All compounds 5 were assayed for inhibitory activity against A549 lung cancer cell growth, and the inhibitory effect of the novel morpholin-3-ones on cell viability was dose-dependent.A series of 4-aryl-6-aryloxymethylmorpholin-3-one derivatives were synthesized very efficiently from readily available starting compounds in two steps. Ring opening reactions of epoxides with aniline compounds on alumina gave corresponding β-aminoalcohols （3）. The resulting β-aminoalcohols were reacted with 2-chloroacetyl chloride to yield the desired 4-aryl-6-aryloxymethylmorpholin-3-one derivatives （5）. All compounds 5 were assayed for inhibitory activity against A549 lung cancer cell growth, and the inhibitory effect of the novel morpholin-3-ones on cell viability was dose-dependent.

关 键 词：morpholin-3-one β-aminoalcohol bioactivity 

分 类 号：O626.4[理学—有机化学] O621.29[理学—化学]