摘要
以2,4,6-三甲基苯甲酰氯为原料合成2,4,6-三甲基苯甲酰乙酸乙酯2a.以水杨醛类化合物与苯甲酰乙酸乙酯类化合物,六氢吡啶为催化剂在乙醇中发生环合反应,合成了8个3-苯甲酰基类化合物4a-4h,所有的化合物只需要重结晶纯化,就能得到纯度较高的目标产物.所有目标化合物均经过^(13)C NMR,^(1 )H NMR,ESI-MS对其进行了结构确认.在412 nm处,通过紫外分光光度测定化合物对乙酰胆碱酯酶和丁酰胆碱酯酶的抑制活性.
2,4,6-trimethylbenzoylacetic acid ethyl ester 2a was obtained from 2,4,6-trimethylbenzoyl chloride.Eight 3-benzoyl compounds 4a-4h are synthesized with cyclization reaction of obtained ethyl benzoylacetate and salicylaldehyde compounds catalyzed by piperidine in ethanol.All the compounds were purified only by recrystallization to obtain higher purity,and were confirmed by 13C NMR,1H NMR and ESI-MS.An inhibitory activity of the compounds on acetylcholinesterase and butyrylcholinesterase was determined by UV spectrophotometry at 412 nm.
作者
胡玉恒
杨洁
孙捷
王晓静
HU Yuheng;YANG Jie;SUN Jie;WANG Xiaojing(School of Medicine and Life Sciences,University of Jinan-Shandong Academy of Medical Sciences,Jinan 250200,Shandong,China;Institute of MateriaMedica,Shandong Academy of Medical Sciences,Jinan 250062,Shandong,China;Key Laboratory for Biotech-Drugs Ministry of Health,Jinan 250062,Shandong,China;Key Laboratoryfor Rare & Uncommon Diseases of Shandong Province,Jinan 250062,Shandong,China)
出处
《化学研究》
CAS
2019年第1期55-60,共6页
Chemical Research
基金
山东省自然科学基金(ZR2018LH021)
