Synthesis, X-ray crystal structure and biological activities of α-phenoxyl-1,2,3-thiadiazoleacetamide
作者:Wei Guang Zhao、Zheng Ming Li、Zhao Yang
DOI:10.1002/jhet.5570400529
日期:2003.9
3-thiadiazole-4-acetamide 4 and was demonstrated by the X-ray crystal structure of its derivative 5a. A novel series of α-substituted phenoxy-N-methyl-1,2,3-thiadiazole-4-acetamide 5 were synthesized through the reaction of the compound 4 and phenols. The results of bioassays show that the title compounds exhibit good anti-HBV activities. The crystal of compound 5a, N-methyl-α-2-bromophenyl-1,2,3-thiadiazole-4-acetamide
1,2,3-噻二唑环的成环反应是通过使带有相邻α-甲基的N-酰基hydr 2a与亚硫酰氯反应而完成的,从而得到α-氯-N-甲基-1,2,3-噻二唑-4-乙酰胺4并通过其衍生物5a的X射线晶体结构证明。通过化合物4与苯酚的反应合成了一系列新的α-取代的苯氧基-N-甲基-1,2,3-噻二唑-4-乙酰胺5。生物测定的结果表明标题化合物具有良好的抗HBV活性。化合物5a,N的晶体已经制备了-甲基-α-2-溴苯基-1,2,3-噻二唑-4-乙酰胺,并通过X射线衍射测定。