762266-07-9

Upstream product

• 82104-74-3 1-oxo-1,3-dihydro-isobenzofuran-5-carbonitrile 
• 352-13-6 4-flourophenylmagnesium bromide 

Downstream Products

• 207680-98-6 4-[(4-fluoro-phenyl)-hydroxy-methyl]-3-hydroxymethyl-benzonitrile 
• 762266-09-1 1,1-bis(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile 
• 64169-67-1 1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile 

Relevant academic research and scientific papers

Preparation method of escitalopram process impurities

The invention relates to a preparation method of escitalopram process impurities. The escitalopram process impurities are obtained by reaction of 5-cyanophthalide with 4-fluorophenylmagnesium bromide.The process is simple and the yield is high.

Preparation method of citalopram intermediate

The invention provides a preparation method of a citalopram intermediate, and belongs to the technical field of pharmaceuticals. In the method, 2-methyltetrahydrofuran is taken as a reaction solvent. Under the protection of nitrogen, a 4-fluorophenylmagnesium bromide solution Grignard reagent, 5-cyanophthalein and a N,N-dimethylpropyl magnesium chloride Grignard reagent are taken as raw materials. A reaction is carried out to synthesize 4-(4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl)-3-(hydroxymethyl)benzonitrilehydrobromide. The method is characterized by high yield and high purity, and is suitable for industrial production.

PROCESS FOR THE PREPARATION OF A CYANO-ISOBENZOFURAN

A process for the preparation of citalopram and the pharmaceutically acceptable salts therof is disclosed by reacting 5-cyanophthalide with a 4-fluorophenyl magnesium halide, reducing the 3-hydroxymethyl-4-(4-fluoro-benzoyl)benzonitrile with an agent reducing ketones to alcohols, submitting the thus-obtained 3-hydroxymethyl-4- [(4-fluorophenyl)hydroxymethyl) benzonitrile to a cyclization reaction to give 1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile without 1,1-bis(4-fluorophenyl)-1,3-dihydro-5- isobenzofurancarbonitrile and treating 1,1-bis(4 fluorophenyl)-1,3-dihydro-5- isobenzofurancarbonitrile with a 3-(dimetylamino)propyl halide in the presence of a base.