SynOpen ( IF 2.0 ) Pub Date : 2023-09-26 , DOI: 10.1055/a-2157-5855 Manjinder Singh Gill 1 , Prachi Ramteke 1
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Efficient, practical syntheses of sorafenib and regorafenib have been achieved in a manner that is free from the problems associated with previously reported methods. The process involved preparation of 4-(4-aminophenoxy)-N-methylpicolinamide (sorafenib intermediate) and 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide (regorafenib intermediate) using only a single base and did not require the use of an inert atmosphere. The reaction of intermediates with phenyl 4-chloro-3-(trifluoromethyl)phenyl carbamate, prepared using water-assisted synthesis of carbamates, was used to install the main urea functionality in these molecules.
中文翻译：
一种实用高效的索拉非尼和瑞戈非尼合成方法
索拉非尼和瑞戈非尼的高效、实用合成已经以不存在与先前报道的方法相关的问题的方式实现。该过程涉及仅使用单一碱制备 4-(4-氨基苯氧基) -N-甲基吡啶酰胺（索拉非尼中间体）和 4-(4-氨基-3-氟苯氧基）-N-甲基吡啶酰胺（瑞戈非尼中间体），并且不需要使用惰性气氛。中间体与通过水辅助氨基甲酸酯合成制备的4-氯-3-(三氟甲基)苯基氨基甲酸酯的反应用于在这些分子中安装主要的脲官能团。
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