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
-
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.
Preparation method of substituted benzobfuran-2-formamide
-
Paragraph 0047; 0048; 0049, (2016/10/08)
The invention belongs to the technical field of medicine, and discloses a preparation method of substituted benzobfuran-2-formamide (please see the formula in the specification). A compound shown in the formula (2) is obtained by removing the protecting group of a compound (3), and then 5-(1-piperazinyl)-benzofuran-2-formamide (1) is obtained through ammonolysis. The method overcomes the defects of an existing preparation method, operation is easy, use of expensive catalysts is avoided, intermediates can be conveniently separated, and cost is low.