2,6-Dihalogenated benzonitrile(1a-b)and morpholine was synthesized to 2-halo-6-(4-morpholinyl)benzonitrile(2a-b) which was cyclized to generate 4-(4-morpholinyl)-1H-indazole-3-amine(3).The effects of the type of base,the reaction solvent,the reaction temperature and the reaction time on the reaction were explored.The results showed that 2-fluoro-6-(4-morpholinyl)ben-zonitrile(2b)was reacted in sodium acetate/DMF system at 70 ℃ for 14 h,the yield of compound 3 could reach 84.5%.%2,6-二卤代苯腈(1a-b)和吗啉反应合成了2-卤代-6-(4-吗啉基)苯腈(2a-b),后者环合生成4-(4-吗啉基)-1H-吲唑-3-胺(3).探索了反应体系中碱的种类、反应溶剂、反应温度以及反应时间对反应的影响,结果表明,2-氟-6-(4-吗啉基)苯腈(2b)在乙酸钠/DMF体系中70 ℃下反应14 h,化合物3的收率可以达到84.5%.
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