Analyzing the synthesis route of

These common heterocyclic compound, 367-22-6, name is 4-Chloro-3-fluoroaniline, its 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. COA of Formula: C6H5ClFN

Description 45 (78 mg, 0.37 mmol) and 3-fluoro-4-chloroaniline (54 mg, 0.37 mmol) inMeCN (2 ml) in the presence of a catalytic quantityof DMAP were stirred at 45 C for 16 h. The reaction was cooled and the resultant solid collected by filtration and rinsed with ether. Without further purification this solid was added to sodium hydroxide solution(1 % aqueous w/w, 2 ml) and heated at 80 OC for 30 min. The reaction was cooled, filtered throughCeliteX to remove insoluble impurities and the filtrate was acidified to pH-6 by the dropwise addition of hydrochloric acid (5N) to precipitate the product. The solid was collected by filtration, rinsed with water then ether and dried to give the title compound (70 mg). 1H NMR (400 MHz, DMSO)8 7.86(1H, s), 7.70(1H, t, J8.4), 7.43(1H, dd,J2. 2,10. 0), 7.14-7. 12(1H, m),3. 77 (3H, s) ;Mlz (ES+) 313,311 (M+H+).

The synthetic route of 4-Chloro-3-fluoroaniline has been constantly updated, and we look forward to future research findings.

Reference:
Patent; MERCK SHARP & DOHME LIMITED; HOLLINGWORTH, Gregory, John; JONES, A., Brian; SPAREY, Timothy, Jason; WO2005/49613; (2005); A1;,
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