- PROCESS FOR PRODUCING HYDROBROMIDE OF DIOL COMPOUND
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PROBLEM TO BE SOLVED: To provide a method for producing 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile hydrobromide with a high purity and a high isolation yield. SOLUTION: Provided is a process for producing 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile hydrobromide characterized in bringing 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile and hydrogen bromide into contact in a mixed solvent of an ester-based solvent and water. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0040-0042
(2020/05/14)
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- METHOD OF PRODUCING CITALOPRAM DIOL COMPOUND
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PROBLEM TO BE SOLVED: To provide a method of producing citalopram diol in a high purity and a high yield. SOLUTION: A production method for obtaining 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile by reacting 5-cyanophtalide with 4-magnesiumbromidefluorobenzene and 3-magnesiumchloride-N,N-dimethyl-1-propaneamine includes: a process of obtaining a solution of 4-magnesiumbromidefluorobenzene using less than 1 mol of magnesium to 1 mol of 4-bromofluorobenzene in an organic solvent; and a process of reacting less than 1 mol magnesium with 1 mol of 3-chloro-N,N-dimethyl-1-propanamine in an organic solvent to obtain a solution of 3-magnesiumchloride-N,N-dimethyl-1-propaneamine. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0050-0058
(2019/10/01)
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- Preparation method of citalopram intermediate
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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.
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Paragraph 0120-0125; 0141- 0147; 0155-0167
(2016/12/01)
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- PREPARATION OF CITALOPRAM AND SALTS THEREOF
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Process for the preparation of citalopram and its salts, comprising reacting magnesium (5-cyano-2-(4-fluorobenzoyl)phenyl)methanolate bromide with 3-N,N-dimethylaminopropyl magnesium halide in a mixture of solvents, obtaining a diol intermediate in the form of its acid addition salt, and reacting the acid addition salt with sulfuric acid in an aqueous medium.
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Page/Page column 4
(2010/04/30)
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