Application of sodium difluorochloroacetate

 Background and overview

Sodium difluorochloroacetate is an off-white solid used as a reagent for organic synthesis, pesticides and pharmaceutical intermediates. 


It has been reported in the literature that it can be used to prepare intermediates such as methyl 3-bromo-4-difluoromethoxybenzoate, 1,3,5-triazine and 3-hydroxy-4-difluoromethoxybenzaldehyde.


Application 1.

CN201210188810.5 discloses a preparation method of methyl 3-bromo-4-difluoromethoxybenzoate shown in formula 3, which comprises the following steps: compound 2, sodium difluorochloroacetate, inorganic weak base After being mixed with an organic solvent, react at a temperature of 85 to 110° C. to get final product;


 the molar ratio of the compound 2, Sodium difluorochloroacetate, inorganic weak base and organic solvent is 1.0: (1.5 to 2.5): ( 1.0~2.0): (15~25); 


The temperature of reaction is 85~110 ​​℃; Described organic solvent is DMF, one or more in isopropanol and 1,4-dioxane; Described The inorganic weak base is one or more of potassium carbonate, cesium carbonate and sodium carbonate. 


The method of the invention has high conversion rate, simple post-processing, high product yield and high purity, and is suitable for industrial production.


Application 2.

CN201910238354.2 discloses a preparation method of multi-substituted 1,3,5-triazine, specifically, using substituted formamidine hydrochloride as a reaction substrate, Sodium difluorochloroacetate as carbon synthon, under the action of an equivalent inorganic base Then, through the cleavage of carbon-chloro, carbon-carbon and carbon-fluorine bonds, a symmetrical or asymmetrical polysubstituted 1,3,5-triazine is obtained; 

The general chemical structure of the substituted formamidine hydrochloride is:


The inorganic base is selected from one of potassium carbonate, sodium carbonate and cesium carbonate. 


The preparation method disclosed in the invention has the advantages of easy availability of raw materials, no need for catalysts and oxidants, a wide range of substrates, simple and convenient operation, green environmental protection and the like.


Application three,

CN201511035182.7 discloses a method for synthesizing 3-hydroxy-4-difluoromethoxybenzaldehyde. 


The method uses 3,4-dihydroxybenzaldehyde as a raw material and uses solid Sodium difluorochloroacetate as a The difluoromethylation reagent can obtain 3-hydroxy-4-difluoromethoxybenzaldehyde in high yield under the action of a base, and the obtained product is an important intermediate for the synthesis of the drug Roflust.

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