103 results about "Vortioxetine" patented technology

The invention discloses a preparation method of vortioxetine (I). The preparation method comprises the following steps: subjecting a compound shown in a formula (II) as a raw material and 2,4-dimethylthiophenol (III) to condensation to generate 2-(2,4-dimethylphenylthioalkyl)nitrobenzene (IV) or 2-(2,4-dimethylphenylthioalkyl)aniline (V) which is obtained by reducing the 2-(2,4-dimethylphenylthioalkyl)nitrobenzene (IV), and subjecting the 2-(2,4-dimethylphenylthioalkyl)aniline (V) and a compound shown in a formula (VI) to cyclization under alkaline conditions to obtain the vortioxetine (I). The preparation method is accessible in raw materials, is concise in process, is economical and environment-friendly and is suitable for industrial production.

The invention discloses a preparation method of vortioxetine (I). The preparation method comprises the following steps: subjecting 2-substituted thiophenol shown in a formula (II) and 2,4-dimethylphenyl halide shown in a formula (III) to condensation to generate 2-(2,4-dimethylphenylthioalkyl)nitrobenzene (IV) or 2-(2,4-dimethylphenylthioalkyl)aniline (V) which is obtained by reducing the 2-(2,4-dimethylphenylthioalkyl)nitrobenzene (IV), and subjecting the 2-(2,4-dimethylphenylthioalkyl)aniline (V) and a compound shown in a formula (VI) to cyclization under alkaline conditions to obtain the vortioxetine (I). The preparation method is accessible in raw materials, is concise in process, is economical and environment-friendly and is suitable for industrial production.

The invention relates to the technical field of medicines and in particular relates to a hydrobromic acid vortioxetine gastric-soluble tablet and a preparation method thereof. The hydrobromic acid vortioxetine gastric-soluble tablet comprises the following components in percentage by weight: 4.24% of hydrobromic acid vortioxetine, 1.0-5.0% of a lubricating agent, 81-91% of a filling agent, 2-5% of a binding agent and 2-15% of a disintegrating agent. Dissolution rate of the hydrobromic acid vortioxetine gastric-soluble tablet is similar to the foreign original standard, so that the hydrobromic acid vortioxetine gastric-soluble tablet has good application prospect and market prospect.

The invention discloses a preparation method and intermediate of vortioxetine. The preparation method of vortioxetine includes the following steps that 1, a compound V is prepared according to a preparation method of the compound V; 2, the compound V and dichloro ethylamine or salt of dichloro ethylamine are subjected to a cyclization reaction in a high-boiling-point solvent to prepare vortioxetine, wherein the boiling point of the high-boiling-point solvent is above 120 DEG C at normal pressure. The preparation method is low in cost, easy to implement, safe, environmentally friendly, high in yield and suitable for industrial production, and reaction conditions are mild.

A process for the manufacture of vortioxetine is provided in which a compound of formula I, formula I is reacted with optionally substituted piperazine and 2,4-dimethylthiophenol(ate) followed by de-cmplexation.

Pharmaceutical compositions comprising vortioxetine and donepezil are provided and the use of such composition for the treatment of cognitive dysfunctions.

The present invention relates to a process for the preparation of 1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine of formula (I), also known as vortioxetine, salts thereof, and intermediates useful for its synthesis.

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.

The invention discloses vortioxetine sustained-release capsules as well as a preparation method and application of the vortioxetine sustained-release capsules. The vortioxetine sustained-release capsules are prepared by loading vortioxetine sustained-release micro-pills into hollow capsules. Each vortioxetine sustained-release micro-pill is composed of a medicine-carrying pill core, an isolation type coating layer, a sustained-release coating layer and a protective coating layer from inside to outside, wherein the medicine-carrying pill core is composed of vortioxetine, an adhesive and a sucrose hollow pill core, and the specific weight percent is as follows: 0.1 percent to 10 percent of the vortioxetine, 10 percent to 30 percent of the adhesive and 10 percent to 60 percent of the sucrose hollow pill core. A sustained-release preparation can be used for prolonging the holding time of treatment concentration of the vortioxetine in a body to 12h and reducing the side effect caused by the fact that the fluctuation of plasma drug concentration is too great; meanwhile, the number of times of orally taking drug is reduced, and the vortioxetine sustained-release capsules have remarkable effect on patients with depressive disorder, who need to be treated, and are convenient to use.

The present invention discloses a hydrobromic acid vortioxetine crystal that has diffraction peaks at 8.55+ / -0.2, 13.05+ / -0.2, 13.44+ / -0.2, 14.46+ / -0.2, 15.20+ / -0.2, 16.63+ / -0.2, 16.94+ / -0.2, 17.22+ / -0.2, 17.85+ / -0.2, 19.83+ / -0.2, 20.43+ / -0.2, 21.33+ / -0.2, 23.14+ / -0.2, 23.60+ / -0.2, 24.77+ / -0.2, 26.25+ / -0.2, 26.72+ / -0.2, 26.96+ / -0.2, 29.69+ / -0.2, 30.52+ / -0.2, 33.33+ / -0.2, 33.89+ / -0.2, 34.89+ / -0.2, 35.54+ / -0.2, 37.03+ / -0.2, and 38.33+ / -0.2 in a powder X-ray diffraction diagram represented with 2 theta. In addition, the present invention further discloses a preparation method for the crystal. The hydrobromic acid vortioxetine crystal and the preparation method therefor in the present invention have good repeatability, easy operation, good product stability, and high yield and purity, and are suitable for industrial production.