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ChemicalBook CAS DataBase List Benzoic acid, 2-amino-4,6-difluoro-, methyl ester (9CI)
379228-57-6

Benzoic acid, 2-amino-4,6-difluoro-, methyl ester (9CI) synthesis

6synthesis methods
-

Yield:379228-57-6 88%

Reaction Conditions:

with potassium carbonate in N,N-dimethyl-formamide at 20; for 2 h;Inert atmosphere;

Steps:

1.2 Step 2: Methyl 2-amino-4, 6-difluoro-benzoate

To a suspension of 2-amino-4,6-difluoro-benzoic acid (94.0 g, 543.0 mmol) and K2CO3 (112.6 g, 814.5 mmol) in DMF (1L) was added iodomethane (92.5 g, 651.6 mmol) dropwise under N2 atmosphere, and the mixture was stirred at 20 °C for 2 h. The mixture was quenched with water (3.5 L), and stirred at 20 °C for 30 min. The suspension was filtered. The cake was washed with 1 L of a solution of a 20: 1 petroleum ether: EtO Ac and dried under vacuum to afford the title compound (89 g, 88%) as brown solid. LCMS: [M+H]+ 188.1.

References:

WO2020/257416,2020,A1 Location in patent:Page/Page column 69