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ChemicalBook CAS DataBase List methyl 3-amino-2-fluorobenzoate

methyl 3-amino-2-fluorobenzoate synthesis

10synthesis methods
-

Yield:1195768-18-3 100%

Reaction Conditions:

with thionyl chloride at 0; for 12 h;Reflux;

Steps:

137

Example 1378-Fluoro-3 ,3 -dimethyl-2- (3 -morpholin-4-yl-phenyl) - 1 ,2,3 ,4-tetrahydro-quinoline-7- carboxylic acid To a stirred solution of 3-amino-2-fiuoro-benzoic acid (25 g, 161 mmol) in methanol (300 mL) was added thionyl chloride (30 mL, 403 mmol) dropewise at 0 °C . Then the mixture solution was refluxed for 12 hours before cooling to room temperature. Then the reaction mixture was concentrated in vacuo and the residue was dissolved in ethyl acetate (500 mL), washed with saturated aqueous sodium bicarbonate solution (3 x 100 mL), dried over anhydrous sodium sulfate and concentrated in vacuo to afford 3-amino-2-fiuoro- benzoic acid methyl ester (27.5 g, quant.) as a pale-white solid: LC/MS m/e calcd for C8H8FN02 (M+H)+: 170.16, observed: 169.9.

References:

WO2011/128251,2011,A1 Location in patent:Page/Page column 230-231

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