Electric Literature of 367-22-6,Some common heterocyclic compound, 367-22-6, name is 4-Chloro-3-fluoroaniline, molecular formula is C6H5ClFN, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
[0216] Ethyl 2-(4-chloro-3-fluorophenylamino)-2-oxoacetate (2′). TEA (2.28g, 0.023 mol) was added at once to a solution of 3 g (0.0206 mol) 4-chloro-3-fluoroaniline in 50 ml of DCM and then ethyl 2-chloro-2-oxoacetate (2.81 g, 0.0206 mol) was added dropwise at 0C. Reaction mixture was stirred at 0C for 1 h and then continued at room temperature (RT) for 6 h. The mixture was washed with 25% aqueous solution of K2C03 (2×50 ml) and water (50 ml). The product was dried over Na2S04 and evaporated. The residue was washed with ether and dried on the air to give ethyl 2-(4-chloro-3-fluorophenylamino)-2- oxoacetate (2′) (3.97 g, 78.6%) as a white powder; LC-MS (APCI+) m/z: calcd for C10H9CIFNO3: 245.03; found: 245 (M+H+).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Chloro-3-fluoroaniline, its application will become more common.
Reference:
Patent; NEW YORK BLOOD CENTER, INC.; THE UNITED STATES OF AMERICA as represented by THE DEPARTMENT OF HEALTH AND HUMAN SERVICES (WASHINGTON, DC); DEBNATH, Asim, Kumar; CURRELI, Francesca; KWONG, Peter, D.; KWONG, Young, Do; WO2013/36676; (2013); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics