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以苯、丁二酸酐为原料,经傅克酰基化,硝化,与水合肼反应三步反应合成6-(3-氨基苯基)-4,5-二氢哒嗪-3(2H)-酮(1),总收率为58.3%.由3-(3-硝基苯甲酰基)丙酸(3)合成化合物1的过程中,在雷尼镍(Raney Ni)的催化下与水合肼反应,一步完成了苯环上硝基的还原和成环.重点考察了该步反应的物料配比、反应时间对产率的影响.结果表明,水合肼与化合物3的摩尔比11.7∶1,回流反应4h,产率为82.7%.

参考文献

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