Method for synthesizing anastrozole intermediate-2,2'-(5-methyl-1,3-phenylene)-bis-(2-methyl propionitrile)
A technology of anastrozole and methylpropionitrile, applied in the field of compound synthesis, can solve the problems of difficult synthesis of starting materials and low yield of intermediates, and achieve the effect of easy synthesis, high yield, and cheap and easy-to-obtain raw materials
Active Publication Date: 2011-02-16
UNIV OF SCI & TECH OF CHINA
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The invention provides a method for synthesizing an anastrozole intermediate-2,2'-(5-methyl-1,3-phenylene)-bis-(2-methyl propionitrile), which comprises the following steps: dissolving a cyanoacetate derivative and 3,5-dihalogenated toluene in a solvent, carrying out decarboxylation cyanomethylation reaction under the action of a palladium catalyst and an organic phosphorus ligand, obtaining a target product, or obtaining 2,2'-(5-methyl-1,3-phenylene)-bis-(acetonitrile), and further being reacted with halogenated methane or methane which is ready to be halogenated in the presence of a strong base hydride, and generating the target product. The method for synthesizing the intermediate can avoid the use of highly toxic cyanide, and has the advantages of cheap price and easy obtainment of raw materials, easy synthesis, no side reactions and high yield.
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