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甲苯咪唑(1)是一个重要的苯并咪唑氨基甲酸酯类的广谱驱虫药。其主要中间体是3,4-二氨基二苯酮(2)系由3-硝基-4-氨基二苯酮还原而得。本文报道从N-苯基氨基甲酸甲酯或N-乙酰苯胺制得2,纯度和收率均高。再经一步反应合成1。 N-苯基氨基甲酸甲酯(或N-乙酰苯胺)在温和条件下用α-三氯甲苯进行苯甲酰化,得相应的二苯酮,收率定量。继用硝酸低温硝化,得到N-(4-苯甲酰基-2-硝基苯基)-氨基甲酸甲酯(或3-硝基-4-乙酰胺基二苯酮),
Mebendazole (1) is an important broad-spectrum de-worming drug for benzimidazole carbamates. Its main intermediate is 3,4-diaminobenzophenone (2) derived from 3-nitro-4-aminobenzophenone derived. This article reports from N-phenyl carbamate or acetanilide prepared 2, both high purity and yield. Then one step reaction synthesis 1. Benzoylation of N-phenylcarbamate (or acetanilide) with α-trichlorotoluene under mild conditions gave the corresponding benzophenone in quantitative yield. Subsequent nitration with nitric acid gave N- (4-benzoyl-2-nitrophenyl) -carbamic acid methyl ester (or 3-nitro-4-acetamidobenzophenone)