These common heterocyclic compound, 2106-04-9, name is 3-Chloro-2-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. category: chlorides-buliding-blocks
To 3-chloro-2-fluoroaniline (10.0 g, 68.7 mmol) in DMSO (500 mL) was added copper (II) chloride (18.5 g, 137.4 mmol) and conc. HCl (50 mL). The whole was heated to 90 C. for 13 h. The reaction was cooled to 0 C. and 4N NaOH was added dropwise to adjust to pH 8. The reaction was diluted with water and extracted with Et2O/EtOAc (1:1). The organic layer was washed with brine, and was dried, filtered and concentrated. The resulting residue was purified via silica gel chromatography eluding with 5-30% EtOAc/hexane to provide 4-amino-2-chloro-3-fluoro-benzaldehyde (1.00 g) as a yellow powder.
The synthetic route of 3-Chloro-2-fluoroaniline has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Nirschl, Alexandra; Sutton, James C.; Hamann, Lawrence; Wang, Tammy; Zou, Yan; Sun, Chongqing; US2005/197359; (2005); A1;,
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