吲唑类化合物合成新方法的研究(Ⅰ)  

Studies on the New Method for Syntheses of IH-Indazoles ( Ⅰ )

作　　者：钟振起[1] 徐潼生[1] 陈小耐[2] 邱玉珠[3] 胡宏纹[3] 

机构地区：[1]河南医科大学有机化学教研室,郑州450052 [2]河南医科大学肿瘤研究所 [3]南京大学化学系

出　　处：《高等学校化学学报》1993年第8期1096-1099,共4页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金

摘　　要：本文研究了2,6-二烷氧基苯乙酮腙在多聚磷酸(PPA)存在下受热脱去一分子醇环化生成3-甲基-4-烷氧基吲唑的合成反应.并研究了水杨醛、邻甲氧基苯甲醛、2,4-二羟基苯甲醛以及邻羟基苯乙酮、2-羟基-3,5-二甲基苯乙酮腙在PPA存在下的受热反应过程.In this paper, we put forward a new and convenient method for the synthesis of 1H-indazoles. In the presence of PPA, the cyclization of a series of 2,6-dialkoxyl (or hydroxy)ace-tophenone hydrazones(2a-f) gave 3-methyl-4-alkoxyl ((?) hydroxy)-1H-indazoles (3a-f). This new method offers several advantages: easy access of the reagents, reasonable yield and short reaction time. We also studied its applied range. The application of this method to 2-methoxy-4,6-dimethylacetophenone hydrazone (2g) gave 3, 4,6-trimethyl-1H-indazole (3g). But the application of it to salicyaldehyde, o-methoxybenzaldehyde, 2,4-dihydroxybenzaldehyde or o-hydroxy-acetophenone, 2-hydroxy-3, 5-dimethylacetophenone hydrazones (2h-l) could not bring about ring closure, resulted in the formation of the corresponding azines (3h-l) in excellent yields.

关 键 词：腙 多聚磷酸 吲唑 吖嗪 

分 类 号：O626[理学—有机化学]