2-(4-β-D-吡喃阿洛糖苷-苯基)-5-取代芳基-1,3,4-噁二唑的合成及镇静活性研究  

Synthesis and Calm Activity of 2-(4-β-D-Allopyranosyloxyphenyl)- 5-substitutedaryl-1,3,4-oxadiazoles

作　　者：李家林[1] 樊波[1] 罗华玲[1] 李颖[1] 尹述凡[1] 

机构地区：[1]四川大学化学学院,成都610064

出　　处：《有机化学》2011年第1期110-114,共5页Chinese Journal of Organic Chemistry

摘　　要：以豆腐果苷为原料,与取代苯甲酰肼反应生成中间体4-β-D-吡喃阿洛糖苷-苯甲醛取代苯甲酰腙(2a～2g),在溴作催化剂的条件下发生关环反应,合成了一系列豆腐果苷类似物3a～3g,所有化合物结构经IR,1H NMR以及MS谱得以证实.初步药理实验结果表明,化合物3a,3c,3f与豆腐果苷相比有更好的镇静活性。A series of novel helicid derivatives containing 1,3,4-oxadiazole 3a-3g were successfully synthesized from the intermediates aryl-3-carbonyl （4-β-D-allopyranoside-yl）-benzaldehyde hydrazone derivatives （2a-2g）, which prepared starting from helicid. The new compounds were characterized by ^1H NMR, IR and HR-MS spectra. The sedative-hypnotic activities of the target compounds 3a-3g were evaluated by testing the spontaneous locomotor activity in mice. All of the derivatives produced moderate to high activities. In particularly, compound 3c presented the most potent sedative-hypnotic effect in comparison to the other derivatives, and compounds 3a and 3f also showed potent activities.

关 键 词：豆腐果苷 镇静活性 1 3 4-噁二唑 合成 环化 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]