New downstream synthetic route of Methyl 3-(2,6-difluorophenylsulfonamido)-2-fluorobenzoate

According to the analysis of related databases, 1195768-19-4, the application of this compound in the production field has become more and more popular.

Synthetic Route of 1195768-19-4, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 1195768-19-4 as follows.

A solution of Lithium bis(trimethylsilyl)amide (1M in THF, l.OlmL, l.Olmmol) was added to a cooled (0C) solution of Methyl 3-((2,6-difluorophenyl)sulfonamido)-2- fluorobenzoate (lOOmg, 0.29mmol) in THF (2.5mL). After lOmin of stirring, a solution of 4-Methyl-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (76mg, 0.29mmol) in THF (lmL) was slowly added and the reaction mixture was allowed to warm to room temperature. After 2 hours of stirring, saturated aqueous ammonium chloride was added to the medium. The aqueous layer was extracted with EtOAc (two times). Combined organics were washed with brine, dried over sodium sulphate, filtered and the filtrate was concentrated under reduced pressure to afford the title compound (170mg, quant) as a mixture of ketone and enol. LC/MS (ES+): 577.4 (M+l).

According to the analysis of related databases, 1195768-19-4, the application of this compound in the production field has become more and more popular.

Reference:
Patent; CELLIPSE; PRUDENT, Renaud; PAUBLANT, Fabrice; (74 pag.)WO2018/55097; (2018); A1;,
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