Preparation of ureido derivative
A urea-based and phenyl-based technology, which is applied in the preparation of urea derivatives, organic compounds, cyanide reaction, etc., can solve the problems of increased production costs and expensive palladium catalysts, etc.
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[0027] 1. Preparation of N-(2-bromo-6-fluorophenyl) alkyl amides
[0028] 1) Add 49.2 g (0.26 mol) of 2-bromo-6-fluoroaniline to a mixed solvent of 492 ml of isopropyl acetate and 180 ml of water, then add 49.2 g of disodium hydrogen phosphate, stir, and then add 42.2 g ( 0.35mmol) pivaloyl chloride was added dropwise to the system, and the reaction system was reacted at room temperature for 3 hours. After the reaction was completed, the layers were separated, and the organic phase was taken. Once, the organic phase was concentrated, and the residue was slurried in n-hexane to obtain a white solid, which was filtered and dried in vacuo to obtain 61.4 g of a solid with a yield of 86.15%.
[0029] 2) Add 38.4 g (0.20 mol) of 2-bromo-6-fluoroaniline to a mixed solvent of 384 ml of isopropyl acetate and 140 ml of water, then add 38.4 g of disodium hydrogen phosphate, stir, and then add 32.9 g ( 0.27mmol) isovaleryl chloride was added dropwise to the system, and the reaction syste...
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