163521-12-8Relevant articles and documents
Preparation method of vilazodone
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Paragraph 0033-0052, (2021/02/06)
The invention relates to a preparation method of vilazodone. The preparation method comprises the steps of by using a compound 1 and a compound 2 as raw materials, carrying out one-step reaction underthe condition that trifluoroacetic acid is used as a solvent to obtain a compound I, namely the vilazodone. Compared with the prior art, the method has the advantages of short reaction route, easy post-treatment, high yield, cheap and easily available reagents used in the reaction, convenient operation, simple post-treatment, low cost, small environmental pollution, and suitableness for industrial production of vilazodone.
Preparation method of vilazodone hydrochloride
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Paragraph 0063; 0069-0077; 0093; 0098-0105; 0116-0120, (2019/02/04)
The invention discloses a preparation method of vilazodone hydrochloride. The preparation method comprises the following steps: (1) in the presence of ammonium hydroxide or ammonium hydroxide and N-methylpyrrolidone, enabling 5-(1-piperazinyl)-benzofuran-2-ethyl formate hydrochloride to be subjected to ammonolysis reaction to obtain 5-(1-piperazinyl)-benzofuran-2-formamide; (2) in the presence ofalkali, enabling the 5-(1-piperazinyl)-benzofuran-2-formamide and 3-(4-chlorobutyl) indole-5-formonitrile to be subjected to nucleophilic substitution reaction to obtain a crude product of vilazodone,wherein the alkali is mixed alkali of sodium iodide, N,N-diisopropylethylamine and triethylamine or 1,8-diazabicycloundec-7-ene; (3) refining the crude product of vilazodone to obtain a refined product of vilazodone; and (4) enabling the refined product of vilazodone to be subjected to salt-forming reaction to obtain the vilazodone hydrochloride. By virtue of the ammonolysis reaction and the nucleophilic substitution reaction, the yield is higher, and the purity is higher; and the yield of the vilazodone hydrochloride is increased.
Vilazodone intermediate preparation method
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Paragraph 0023; 0037; 0038; 0039, (2016/11/14)
The present invention provides a vilazodone intermediate preparation method. According to the method, a caproaldehyde compound is adopted as a starting material, and reacts with a phenylhydrazine or aniline compound, and the obtained compound is subjected to ring closure under catalysis of an acid to obtain 3-(4-chlorobutyl)-5-cyano indole. According to the present invention, the application of the acylation reaction catalyzed through the Lewis acid in the literature is avoided, and the step of the methylene obtaining through carbonyl reduction with red aluminum in the literature is avoided and is not easily achieved in the workshop; and the compound is the key vilazodone synthesis intermediate, and the method has characteristics of easily available raw materials, mild reaction condition, simple operation, easy process control, low cost, and easy industrial production.