Development of a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl) nicotinate: trifluoromethylation on kilogram scale

…, X Sun, TG Tampone, J Gao, M Sarvestani…

文献索引：Mulder, Jason A.; Frutos, Rogelio P.; Patel, Nitinchandra D.; Qu, Bo; Sun, Xiufeng; Tampone, Thomas G.; Gao, Joe; Sarvestani, Max; Eriksson, Magnus C.; Haddad, Nizar; Shen, Sherry; Song, Jinhua J.; Senanayake, Chris H. Organic Process Research and Development, 2013 , vol. 17, # 6 p. 940 - 945

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被引用次数: 20

摘要

Reported herein is a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl) nicotinate, an intermediate in the synthesis of novel anti-infective agents. The key to this process is the trifluoromethylation of an aryl iodide using an inexpensive methyl chlorodifluoroacetate (MCDFA)/KF/CuI system, with an emphasis on the development work which led to this effective process.