An Improved Kilogram-Scale Synthesis of 2-Bromo-4-nitro-1H-imidazole: A Key Building Block of Nitroimidazole Drugs

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• 作者：Srinivasa Rao Pedada ; Vijay S. Satam ; Pawan J. Tambade ; Srinivas A. Kandadai ; Rama Mohan Hindupur ; Hari N. Pati ; Delphine Launay ; Denis Martin
• 刊名：Organic Process Research & Development
• 出版年：2013
• 出版时间：September 20, 2013
• 年：2013
• 卷：17
• 期：9
• 页码：1149-1155
• 全文大小：342K
• 年卷期：v.17,no.9(September 20, 2013)
• ISSN：1520-586X

文摘

An efficient two-step method for the synthesis of 2-bromo-4-nitroimidazole, 6, a key building block for nitroimidazole drugs, has been developed. The synthesis involves dibromination of 4-nitroimidazole 10 followed by selective debromination using in situ reductive deiodination strategy. The reactions are facile, safe, and easy to scale up. The large-scale applicability of this improved method was tested by conducting the reactions on kilogram scale to produce the desired product in high yield and quality.