1011-13-8Relevant articles and documents
Application of heterocyclic substituted phenylpiperazine (Phenylpiperidine) derivative in antidepressant drug
-
, (2021/01/24)
The invention discloses application of a heterocyclic substituted phenylpiperazine (Phenylpiperidine ) derivative in an antidepressant drug, and the compound provided by the invention has good inhibitory activity on 5-HT reuptake, 5-HT1A and 5-HT7 recepto
Preparation method of vortioxetine
-
Paragraph 0033; 0047-0048; 0053-0054; 0059-0060; 0065-0066, (2019/10/01)
The invention relates to the field of medicines, in particular to a preparation method of vortioxetine. The preparation method comprises the steps that 2-bromoiodobenzene, N-phenoxycarbonyl piperazineand tert butyl alcohol are subjected to condensation to form an intermediate 1, that is a mixture of 4-(2-bromine phenyl) piperazine-1-tertiary butyl carboxylate and 1-(2-bromine phenyl) piperazine;the intermediate 1 and 2,4-dimethyl phenylthiophenol are subjected to condensation to form an intermediate 2, that is a mixture of N-Boc-vortioxetine and vortioxetine; the N-Boc-vortioxetine in the intermediate 2 is subjected to Boc protecting group removal, and then a crude vortioxetine product is formed through alkalization, and the crude vortioxetine product is subjected to salinization, purification and alkaline dissociation to obtain the vortioxetine. The method has the advantages that the raw materials are simple and easy to obtain, the product has high yield and high purity, and the method is suitable for industrial production.
Method for preparing vortioxetine
-
Paragraph 0011; 0027; 0031; 0035, (2017/08/30)
The invention discloses a method for preparing vortioxetine. The preparation method comprises the following steps: enabling 2-bromobenzenamine to react with sodium nitrite so as to obtain a reactive intermediate in the presence of concentrated sulfuric acid; carrying out a reaction with piperazine to obtain an intermediate A, performing alkali regulation on the intermediate A, and synthesizing with 2,4-dimethylthiophenol, thereby obtaining the target product vortioxetine. The method is short in synthetic route, simple in process, high in product yield, and suitable for industrialized production. The structural formula is as shown in the specification.