Development of a safe and economical synthesis of methyl 6-chloro-5-(trifluoromethyl)nicotinate: Trifluoromethylation on kilogram scale
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.
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.
AROMATIC RING DERIVATIVE AS IMMUNOREGULATION AND PREPARATION METHOD AND APPLICATION OF AROMATIC RING DERIVATIVE
Relating to a compound represented by formula (I) and a pharmaceutically acceptable salt of the compound, and an application of the compound as an S1P1 agonist.
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(2021/10/15)
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