皮斐松-α衍生物的合成及表征  

Synthesis and Characterization of Pifithrin-α Derivatives

作　　者：李海峰[1] 欧阳红霞 陈志军[1] 吕巧莉 Li Haifeng;Ouyang Hongxia;Chen Zhijun;LV Qiaoli(Depatment of Nuclear Medicine,Jiangxi Cancer Hospital,Department of Jiangxi Key Laboratory of Translationl Cancer Research,Nanchang,Jiangxi 330029,China;Fuzhou Medical College of Nanchang University,Fuzhou,Jiangxi 344000,China)

机构地区：[1]江西省肿瘤医院核医学科,江西省肿瘤转化医学重点实验室,江西南昌330029 [2]南昌大学抚州医学院,江西抚州344000

出　　处：《化学世界》2021年第2期112-115,共4页Chemical World

基　　金：国家自然科学基金(No.81860664);江西省卫生健康委基金(Nos.20203566,20175418)资助项目。

摘　　要：以皮斐松-α(PFT-α)为先导化合物,对其结构进行分析、修饰,保留了PFT-α结构中的2-氨基噻唑基本结构母环,设计合成了5种新型PFT-α衍生物Ⅲa~Ⅲe。以无水乙醇为溶剂,在哌啶-冰醋酸存在条件下与不同的醛进行反应,得到目标化合物Ⅲa~Ⅲe,通过IR,^(1)H NMR等对产物、中间体结构进行了表征。The structure of the lead compound of Pifithrin-α(PFT-α) was analysed and modified, five novel Pifithrin-α derivatives were designed and synthesized with Schiff base and 2-thiazolamine ring as the core structure. Five kinds of novel Pifithrin-α derivatives Ⅲa~Ⅲe were synthesized using 2-amino-4,5,6,7-tetrahydro-1,3-benzothiazole and different aldehydes as raw materials in the presence of hexahydropyridine-glacial acetic acid. The reaction conditions of catalyst were optimized and the structures were confirmed by ^(1)H NMR and IR etc.

关 键 词：PFT-Α 合成及表征 神经退行性疾病 

分 类 号：O621.256.4[理学—有机化学]