183288-46-2Relevant articles and documents
Amidation and N-boc deprotection process improvement for the preparation of 5-(1-Piperazinyl)benzofuran-2-carboxamide, a key intermediate of vilazodone
Das, Prasenjit,Srivastava, Bindu,Joseph, Sony,Nizar, Hashim,Prasad, Mohan
, p. 665 - 667 (2014)
An improved process for the preparation of 5-(1-piperazinyl)benzofuran-2- carboxamide, a key intermediate used in the synthesis of antidepressant drug vilazodone is reported.
Preparation method of vilazodone hydrochloride
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Paragraph 0063-0068; 0090-0092; 0093-0097, (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.
Intermediates for preparing [...] 5-piperazinyl-2-acyl substituted benzofuranacetic method (by machine translation)
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Paragraph 0047, (2016/10/07)
The invention discloses a method for preparing a vilazodone intermediate 5-piperazinyl-2-acyl substituted benzofuran. By the method, a corresponding vilazodone intermediate 5-piperazinyl-2-acyl substituted benzofuran is obtained by performing a coupling reaction on 5-halogen-substituted-2-acyl substituted benzofuran and piperazine under the actions of copper serving as a catalyst and a suitable solvent. The invention provides a new method for preparing the vilazodone intermediate 5-piperazinyl-2-acyl substituted benzofuran, has the advantages of short course, conveniences in synthesis, high yield, low cost and the like, and is suitable for industrial production.