ethyl 2,2-difluoro-2-(6-fluoro-2-methyl-2H-indazol-5-yl)acetate synthesis

6synthesis methods

Product Name:ethyl 2,2-difluoro-2-(6-fluoro-2-methyl-2H-indazol-5-yl)acetate
CAS Number:1440965-40-1
Molecular formula:C12H11F3N2O2
Molecular Weight:272.2231

ethyl 2,2-difluoro-2-(6-fluoro-1H-indazol-5-yl)acetate

1440965-39-8
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420-37-1 Synthesis

420-37-1
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ethyl 2,2-difluoro-2-(6-fluoro-2-methyl-2H-indazol-5-yl)acetate

1440965-40-1
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Yield:1440965-40-1 59%

Reaction Conditions:

in ethyl acetate at 20;

Steps:

C1.6 Ethyl 2-(6-fluoro-2-methyl-lH-indazol-5-yl)-2,2-difluoroacetate

Ethyl 2-(6-fluoro-2-methyl-lH-indazol-5-yl)-2,2-difluoroacetate To a 100 mL round bottom flask is added ethyl 2-(l-acetyl-6-fluoro-lH-indazol-5-yl) -2,2- difluoroacetate (1.40 g, 5.4 mmol), ethyl acetate (40 mL), and trimethyloxonium tetrafluorob orate (1.2 g, 8.1 mmol). The reaction mixture is stirred at room temperature overnight. Then aqueous saturated sodium hydrosulfite solution (50 mL) is added. The aqueous phase is isolated and extracted with ethyl acetate (2 X 40 mL). The combined organic phases are washed with brine (50 mL), dried over anhydrous sodium sulfate, and concentrated. The residue is purified on a silica gel flash chromatography with ethyl acetate/petroleum ether (1 :3) to get a yellow solid (1.3 g, 59% yield). (MS: [M+l] 273)

References:

WO2014/32498,2014,A1 Location in patent:Page/Page column 24

307306-08-7 Synthesis