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Synthesis and analysis of 1-methyl-4-phenyl-1H-imidazol-2-amine
Journal of Chemical Research ( IF 1.0 ) Pub Date : 2018-12-01 , DOI: 10.3184/174751918x15414286606248
Qifan Zhou 1 , Fangyu Du 1 , Yajie Shi 1 , Ting Fang 1 , Guoliang Chen 1
Affiliation  

A practical synthetic route to an important pharmaceutical intermediate 1-methyl-4-phenyl-1H-imidazol-2-amine, via a three-step sequence involving cyclisation, hydrolysis and methylation, is reported. In the process of optimisation, a novel chemical entity was isolated and confirmed to be 2,6-diphenyl-1H-imidazo[1,2-a]imidazole by MS, 1H NMR and 13C NMR. The scale-up experiment was carried out to provide 1-methyl-4-phenyl-1H-imidazol-2-amine in 27.4% total yield.

中文翻译:

1-甲基-4-苯基-1H-咪唑-2-胺的合成与分析

报道了一种重要的药物中间体 1-甲基-4-苯基-1H-咪唑-2-胺的实用合成路线,通过涉及环化、水解和甲基化的三步序列进行。在优化过程中,分离出一种新的化学实体,并通过MS、1H NMR和13C NMR证实为2,6-二苯基-1H-咪唑并[1,2-a]咪唑。进行放大实验以提供 1-甲基-4-苯基-1H-咪唑-2-胺,总产率为 27.4%。
更新日期:2018-12-01
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