61337-89-1Relevant articles and documents
A rice the nitrogen is mellow synthetic method
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, (2017/08/25)
The invention discloses a 1-(3-hydroxymethylpyridine-2-yl)-4-methyl-2-phenylpiperazine synthesis method. The method includes: dissolving N-(2-chloroethyl)-N-methyl-alpha-chlorine-beta phenethylamine in mixed solution of water and a nonpolar solvent to obtain solution A, and dissolving 2-amino-3-hydroxymethylpyridine into a nonpolar solvent containing a small quantity of low carbon alcohols to obtain solution B; dripping the solution B into the solution A to obtain an intermediate by reaction, dissolving the intermediate into an anhydrous high-boiling-point polar solvent, and dripping into an anhydrous high-boiling-point polar solvent of inorganic iodides under inert gas shielding to realize reaction for obtaining 1-(3-hydroxymethylpyridine-2-yl)-4-methyl-2-phenylpiperazine. By two steps for synthesis of 1-(3-hydroxymethylpyridine-2-yl)-4-methyl-2-phenylpiperazine, oxidization of the intermediate due to direct high-temperature reaction can be avoided by specific solvent systems, and reaction stability and yield are improved.
MANUFACTURING METHOD OF MIRTAZAPINE
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Paragraph 0060; 0061, (2017/07/14)
PROBLEM TO BE SOLVED: To provide a method for manufacturing mirtazapine useful as an antidepressant at high quality and high manufacturing yield. SOLUTION: Mirtazapine with reduced impurities is manufactured by crystallizing mirtazapine by using a mixed solvent of a good solvent selected from an alcohol solvent, a ketone solvent, an ether solvent and an ester solvent and a poor solvent selected from heptane and hexane, or a mixed solvent of a good solvent and a poor solvent in which a good solvent which is acetonitrile and a poor solvent which is water in a method of manufacturing mirtazapine by reacting 2-(4-methyl-2-phenyl-1-piperazinyl)-3-pyridinemethanol and sulfuric acid. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
METHOD FOR PRODUCING MIRTAZAPINE
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Paragraph 0053; 0054, (2017/10/27)
PROBLEM TO BE SOLVED: To provide a method in which mirtazapine useful as an antidepressant can be produced at high quality as well as at high production yield. SOLUTION: In a method for producing mirtazapine by reacting 2-(4-methyl-2-phenylpiperazin-1-yl)-3-pyridinemethanol with sulfuric acid, when an alcohol solution of crude mirtazapine obtained as a concentrated residue of a toluene extraction liquid is subjected to activated carbon treatment, the amount of toluene is made 15 g or less with respect to 100 g of the alcohol solution, whereby the reduction efficiency of specific impurities during the activated carbon treatment can be improved, and as a result, mirtazapine with high quality can be produced. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT