摘要
探索了一种快速、高效的超声合成方法,通过三组分一锅法合成了20个2'-氨基-2-氧代-5'H-螺[吲哚啉-3,4'-苯并噻喃[4,3-b]吡喃]-3'-甲腈类结构新颖的螺吲哚化合物.所得到的化合物均由1H NMR,13C NMR和HRMS确证.研究了超声对产率和反应时间的影响.采用微量稀释法对所合成的化合物进行了抗真菌活性的测定.其中,化合物4f对新生隐球菌、絮状表皮癣菌和总状毛霉的抑制活性均优于阳性对照药物氟康唑.
A rapid and efficient ultrasound-promoted one-pot synthesis of 2＇-amino-2-oxo-5＇H-spiro[indoline-3,4＇-thiochromeno[4,3-b]pyran]-3＇-carbonitrile compounds by one-pot three-component reaction had been developed. Structures of all products were characterized by 1H NMR, 13 C NMR and HRMS. The effect of ultrasound on yield and reaction time had been studied to understand the role of ultrasound in the reaction. The antifungal activity was determined by micro dilution method. Compound 4f exhibited inhibitory activity to Cryptococcus neoformans, Epidermophyton floccosum and Mucor racemosus better than the positive control drug fluconazole.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2016年第1期143-150,共8页
Chinese Journal of Organic Chemistry
基金
河北省药物质量分析控制重点实验室开放基金
"重大新药创制"国家科技重大专项(No.2012ZX09103-101-057)资助项目~~
关键词
硫色满酮
超声
螺吲哚
三组分一锅法
抗真菌活性
thiochromanone
ultrasound
spirooxindole
one-pot three-component reaction
antifungal activity
