- PROCESS AND NOVEL POLYMORPHIC FORM OF VORTIOXETINE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
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Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is disclosed. A novel crystalline form of vortioxetine hydrobromide propylene glycol solvate, designated form AC1, is disclosed along with a method for making same. Form AC1 may be characterized by an x-ray powder diffraction pattern with peaks at about 19.64, 22.85, 25.51, 29.57, 30.18±0.2 degrees 2-theta.
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- AN IMPROVED PROCESS FOR THE PREPARATION OF VORTIOXETINE AND SALTS THEREOF
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The present invention relates to a novel crystalline polymorphic form of 1-[2-(2,4-dimethyl- phenylsulfanyl)-phenyl]-piperazine hydrochloride; commonly known as vortioxetine hydrochloride (hereafter referred to as the compound (Ia) and process for its preparation comprising of treating the compound (Ia) (as described herein) with a ketone solvent or mixture of ketone solvent with other solvents. The present invention also relates to an improved process for the preparation of vortioxetine hydrobromide (Ia), comprising reacting the compound (I) (as described herein) with hydrogen bromide solution in acetic acid.
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Page/Page column 13
(2019/08/29)
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- AN IMPROVED PROCESS FOR PREPARATION AND PURIFICATION OF VORTIOXETINE HYDROBROMIDE
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The present invention is related to an improved process for the preparation and purification of crystalline polymorph of Vortioxetine hydrobromide of Formula-I and Vortioxetine hydrochloride of Formula-Ia. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.
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Page/Page column 9; 10
(2018/09/19)
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- 1-[2-(2,4-dimethylphenylsulfydryl)phenyl]piperazine hydrochloride and preparation method thereof
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The invention discloses 1-[2-(2,4-dimethylphenylsulfydryl)phenyl]piperazine hydrochloride and a preparation method thereof. By means of the specific preparation method, the HPLC purity of vortioxetinehydrochloride is higher than 99.5%, and the content of
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- PROCESS FOR THE PREPARATION OF VORTIOXETINE AND SALTS THEREOF
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The present invention provides an improved process for preparation of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine; commonly known as vortioxetine (referred to as the compound (I)) and pharmaceutically acceptable salts thereof; wherein the process comprises reaction of 2-((2,4-dimethylphenyl)thio)aniline (II) with bis(2-alkyl)amine (IIIa) or its salt in the presence of a cyclic amide solvent.
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Paragraph 0067
(2018/08/30)
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- Hydrochloric acid [...][...] crystalline hydrochloride monohydrate and its preparation method
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The invention discloses a vortioxetine hydrochloride crystal substance and a preparation method thereof, including three new crystal forms of vortioxetine hydrochloride and preparation methods thereof and application to preparation of medicines for treati
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Paragraph 0100 - 0117
(2018/04/01)
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- Mechanism and Scope of Base-Controlled Catalyst-Free N-Arylation of Amines with Unactivated Fluorobenzenes
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A general method for transition metal-free N-arylation of amines has been developed. Mechanistic studies have revealed that the ability of the base to facilitate the desired amination without promoting unwanted side reactions is the guiding factor. By employing lithium bis(trimethylsilyl)amide as a base the resultant deprotonated amines readily react with a range of unactivated fluorobenzene derivatives. This new arylation method is utilized for the simple two-step synthesis of the antidepressant Vortioxetine.
- Borch Jacobsen, Christian,Meldal, Morten,Diness, Frederik
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p. 846 - 851
(2017/02/05)
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- A PROCESS FOR PREPARATION OF VORTIOXETINE AND POLYMORPHS THEREOF
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The present invention relates to an improved process for preparation of vortioxetine or pharmaceutically acceptable salts thereof. The present invention also relates to new process for the preparation of vortioxetine or pharmaceutically acceptable salts thereof. The present invention further relates to novel polymorphs of vortioxetine hydrobromide and process for preparation thereof.
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- PROCESSES FOR THE PREPARATION OF VORTIOXETINE HYDROBROMIDE
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The present invention relates to a process for the preparation of vortioxetine and its pharmaceutically acceptable salts.
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Page/Page column 35
(2016/09/22)
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- SYNTHESIS OF VORTIOXETINE VIA (2-(PIPERAZINE-1 -YL)PHENYL)ANILINE INTERMEDIATES
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The present invention provides a new synthetic process for the production of 1-(2-((2,4- dimethylphenyl)thio)phenyl)piperazine (vortioxetine), a drug for the treatment of depression and anxiety, which is conducted via (2-(piperazine-1-yl)phenyl)aniline intermediates.
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Page/Page column 19-20
(2015/08/03)
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- NEW PROCESS FOR THE SYNTHESIS OF 1-(2-((2,4-DIMETHYLPHENYL)THIO)PHENYL)PIPERAZINE
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The present invention provides a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine), an experimental drug under development for the treatment of depression and anxiety, which comprises the reaction of a compound of formula (VII), or salt thereof, (VII) wherein Q represents S, SO or SO2 and LG represents a leaving group, with a compound of formula (XI), or salt thereof, (XI) wherein Z represents hydrogen or a protecting group. New intermediate compounds are also provided.
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- NEW PROCESS FOR THE SYNTHESIS OF 1-(2-((2,4-DIMETHYLPHENYL)THIO)PHENYL)PIPERAZINE
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The present invention provides new intermediate compounds or formulae (III) and (IVa), and salts thereof, and their use in a new synthetic process for the production of 1-(2-((2,4- dimethylphenyl)thio)phenyl)piperazine (vortioxetine) an experimental drug under development for the treatment of depression and anxiety.
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- Discovery of 1-[2-(2,4-Dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): A Novel Multimodal Compound for the Treatment of Major Depressive Disorder
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Figure Presented. The synthesis and structure-activity relationship of a novel series of compounds with combined effects on 5-HT3A and 5-HT1A receptors and on the serotonin (5-HT) transporter (SERT) are described. Compound 5m (Lu AA2
- Bang-Andersen, Benny,Ruhland, Thomas,J?rgensen, Morten,Smith, Garrick,Frederiksen, Kristen,Jensen, Klaus Gjervig,Zhong, Huailing,Nielsen, S?ren M?ller,Hogg, Sandra,M?rk, Arne,Stensb?l, Tine Bryan
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supporting information; experimental part
p. 3206 - 3221
(2011/07/08)
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- NOVEL THERAPEUTIC USES OF 1-[2-(2,4-DIMETHYLPHENYLSULFANYL)PHENYL]PIPERAZINE
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The use of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine in the treatment of pain and residual symptoms in depression is provided.
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Page/Page column 18-19
(2008/12/07)
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- 1- [2- (2, 4-DIMETHYLPHENYLSULFANYL) -PHENYL] PIPERAZINE AS A COMPOUND WITH COMBINED SEROTONIN REUPTAKE, 5-HT3 AND 5-HT1A ACTIVITY FOR THE TREATMENT OF COGNITIVE IMPAIRMENT
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1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine exhibits potent activity on SERT, 5-HT3 and 5-HT1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.
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