Development of a Safe and Economical Synthesis of Methyl 6-Chloro-5-(trifluoromethyl)nicotinate: Trifluoromethylation on Kilogram Scale

详细信息    查看全文

• 作者：Jason A. Mulder ; Rogelio P. Frutos ; Nitinchandra D. Patel ; Bo Qu ; Xiufeng Sun ; Thomas G. Tampone ; Joe Gao ; Max Sarvestani ; Magnus C. Eriksson ; Nizar Haddad ; Sherry Shen ; Jinhua J. Song ; Chris H. Senanayake
• 刊名：Organic Process Research & Development
• 出版年：2013
• 出版时间：June 21, 2013
• 年：2013
• 卷：17
• 期：6
• 页码：940-945
• 全文大小：228K
• 年卷期：v.17,no.6(June 21, 2013)
• ISSN：1520-586X

文摘

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.