Electric Literature of 280566-45-2 ,Some common heterocyclic compound, 280566-45-2, molecular formula is C7H3ClF3NO2, 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.
Intermediate 242-Amino-6-(trifluoromethyl)nicotinic acidA solution of 2-chloro-6-(trifluoromethyl)nicotinic acid (1.87 g, 8.29 mmol) in (2,4- dimethoxyphenyl)methanamine (2.491 ml, 16.58 mmol) was heated to 100 0C overnight. The reaction mixture was concentrated under vacuum and partitioned between water and DCM. Evaporation of the organic layer provided a dark brown residue, which was dissolved in TFA (2.55 ml, 33.16 mmol), and the resulting mixture was stirred for 30 minutes. The precipitate formed was discarded via filtration and concentration of the filtrate under reduced pressure gave a residue. This residue was dissolved in HCl (IN, 200 mL) and the aqueous solution was washed with Et2O and evaporated under reduced pressure to give a solid. This solid was washed with DCM/Hexanes, dried in a vacuum oven overnight and characterized as the title product (2 g). LCMS: 207.0 [M+H]+.
In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 280566-45-2, 2-Chloro-6-(trifluoromethyl)nicotinic acid, other downstream synthetic routes, hurry up and to see.
Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; CHUAQUI, Claudio, Edmundo; HUANG, Shan; IOANNIDIS, Stephanos; SHI, Jie; SU, Mei; SU, Qibin; WO2010/38060; (2010); A1;,
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