摘要
通过水解、环合、还原和酸化四步一锅法合成了α-硫辛酸,整个工艺(包括后处理)以水为溶剂,少量乙醇为助溶剂,摒弃了文献工艺中用到的甲苯、乙酸乙酯和环己烷等有机溶剂,因而是一条简便、绿色且具有工业化前景的合成路线。在此基础上以α-硫辛酸为原料合成一系列α-硫辛酸酰肼衍生物,通过元素分析、1H NMR、IR和MS对这些化合物进行了表征;并进一步将此类化合物进行体外人白血病细胞株HL-60、人肺癌A549、人乳腺癌MCF-7、人子宫颈癌细胞株Hela抗肿瘤活性的测试,以顺铂为对照,发现此类化合物对人肺癌A549细胞株具有一定的体外抗肿瘤活性,值得进一步研究。
The synthetic route of α-lipoic acid was improved through four steps of hydrolyzation, cyclization, reduction and acidification. The whole process that based on water as solvent and ethanol as co-solvent, which abandoned the organic solvent of toluene, ethyl acetate and cyelohexane etc. reported in literatures, is a convenient, green synthetic route with the prospect of industrialization. A series of α-lipoic acid acylhydrazine derivatives were synthesized and characterized by IH NMR, MS, IR and element analysis. Furthermore, these compounds were evaluated for their in vitro anticancer activities against HL-60, A-549, MCF-7, Hela cell lines （cisplatin as a control） , and found them with a certain anticancer activities to A-549 cell line. So as-sythesized compounds possess potential antitumor activities and are worthy of further study.
出处
《化学通报》
CAS
CSCD
北大核心
2012年第9期837-841,共5页
Chemistry
基金
2011浙江省大学生科技创新项目(2011R460006)
浙江省台州市科技计划项目(Y201018289)资助
关键词
Α-硫辛酸
酰肼
抗肿瘤活性
合成
α-Lipoic acid, Acylhydrazine, Antitumor activity, Synthesis
