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以豆腐果苷为原料,与盐酸羟胺缩合反应生成4-β-D-吡喃阿洛糖苷-苯甲醛肟(2),2与次氯酸叔丁酯发生取代反应生成4-β-D-吡喃阿洛糖苷-α-氯苯甲醛肟(3);再将3与Schiff碱通过1,3-偶极环加成生成一系列3-(4-β-D-吡喃阿洛糖苷-苯基)-4-芳基-5-芳基-1,2,4-噁二唑啉(5a～5h).3和5a～5h共9个化合物均未见文献报道,其结构经1HNMR,IR和MS(HRMS)加以确认,并对5a～5h进行了药理活性筛选.结果表明,部分化合物具有良好的镇静活性.其中,化合物5g(200,100mg?kg-1)和5h(200,100mg?kg-1)与豆腐果苷相比较具有更强的活性.
Using tofuoside as the raw material, the product is condensed with hydroxylamine hydrochloride to generate 4-β-D-allylidene glycoside-benzaldehyde oxime (2). The substitution reaction between 2 and tert-butyl hypochlorite generates 4-β- Pyraloxaloside-α-chlorobenzaldehyde oxime (3). A series of 3- (4-β-D-allopyranoside- Phenyl-4-aryl-5-aryl-1,2,4-oxadiazolines (5a ~ 5h) .9 and 5a ~ 5h all 9 compounds were not reported in the literature, the structure by 1HNMR, IR and MS (HRMS), and the pharmacological activities of 5a ~ 5h were screened.The results showed that some of the compounds had good sedative activity, among which 5g (200,100 mg? Kg-1) and 5 h -1) is more active than tofuin.