80 results about "Vortioxetine Hydrobromide" patented technology

The invention discloses a preparing method for a vortioxetine hydrobromide alpha crystal form. The preparing method comprises the following step that sec-butyl alcohol is removed from a vortioxetine hydrobromide-sec-butyl alcohol complex to obtain the vortioxetine hydrobromide alpha crystal form. The method is low in desolvation temperature, and the prepared vortioxetine hydrobromide alpha crystal form is high in purity, suitable in particle size and suitable for industrial production.

The invention discloses a vortioxetine hydrobromide crystal preparation method. The method comprises a, dissolving vortioxetine free alkali in ethyl acetate at a temperature of 20-30 DEG C, b, carrying out filtration, cooling the filtrate to a temperature of 0-10 DEG C, dropwisely adding an ethyl acetate solution of hydrobromic acid into the filtrate along with thermal insulation and then carrying out thermal insulation stirring for 2-8h, c, filtering the mixture subjected to thermal insulation stirring in the step b to obtain filter cake 1, leaching the filter cake 1 by ethyl acetate, and carrying out stirring washing in ethyl acetate at a temperature of 0-10 DEG C for 0.5-5h, d, filtering the mixture subjected to stirring washing in the step c to obtain filter cake 2, leaching the filter cake 2 by methyl tert-butyl ether / ethyl acetate pre-cooled at a temperature of 0-10 DEG C and carrying out stirring washing in methyl tert-butyl ether at a temperature of 10-30 DEG C for 15-24h, and e, filtering the mixture subjected to stirring washing in the step d to obtain filter cake 3, leaching the filter cake 3 by methyl tert-butyl ether and carrying out vacuum drying at a temperature of 40-50 DEG C to obtain the product. The method has the advantages of good repeatability, simple processes, a high yield and high product purity and is suitable for industrial production.

The present invention relates to novel crystalline forms of vortioxetine hydrobromide, in particular three crystalline forms, a process for their preparation, a pharmaceutical composition containing said novel crystalline forms, and a process for the purification of vortioxetine or a salt thereof, comprising the formation of one or more of the novel crystalline forms of vortioxetine hydrobromide described herein.

The present invention provides polymorphic forms of Vortioxetine of and its pharmaceutically acceptable salts. Specifically the present invention relates to the novel crystalline forms of Vortioxetine or its pharmaceutically acceptable salts. Moreover, the present invention also provides an amorphous form of Vortioxetine hydrobromide and a stable amorphous co-precipitate of Vortioxetine hydrobromide with pharmaceutically acceptable excipients.

The present invention is directed to a crystalline compound comprising a hydrobromide acid (HBr) salt of a compound of formula (I) (1-{2-[(2,4-dimethylphenyl)sulfanyl]phenyl}piperazine, INN: vortioxetine), having an XRPD pattern with characteristic peaks (expressed in 2θ±0.2° 2θ (CuKα radiation)) at 5.5°, 14.8°, 16.7° and 20.0° and processes for obtaining the same.

The invention discloses a preparation method of an alpha crystal form of vortioxetine hydrobromide. The alpha crystal form, obtained with the method, of vortioxetine hydrobromide has high purity, goodcrystallinity, high stability and particle uniformity. The preparation process is simple, good in repeatability, high in yield and suitable for industrial production.

The invention provides a vortioxetine hydrobromide preparation method. The vortioxetine hydrobromide preparation method comprises the following steps: a reaction is performed between o-bromoiodobenzene and 2,4-dimethylbenzenethiol in a protonic solvent under the action of a cuprous catalyst, glycol and inorganic base to obtain 2-(2,4-dimethylthiophenyl) bromobenzene (a compound IV); the compound IV in an aprotic solvent is coupled with piperazine under the action of a palladium catalyst, a phosphine ligand and organic base; finally, salifying is performed with hydrobromic acid to obtain vortioxetine hydrobromide. Compared with the prior art, the vortioxetine hydrobromide preparation method has the advantages that competition side reactions of dual halogens are avoided, by-products are reduced, the total yield and product purity are high, and the process operation is simple, and suitable for amplification and industrialized production.

The invention belongs to the field of analytical chemistry. The invention discloses an analysis method for separating and determining a vortioxetine hydrobromide intermediate and its isomers by usingliquid chromatography. The method uses a chromatographic column filled with phenyl bonded silica gel as a filler and a certain proportion of a buffer salt solution-organic phase as a mobile phase, andcan quantitatively determinethe content of the vortioxetine hydrobromide intermediate and isomers thereof so that the mass of a vortioxetine hydrobromide starting material is effectively controlled,side reactions are reduced, and therefore it is guaranteed that the quality of a vortioxetine hydrobromide final product is controllable. The method is strong in specificity, high in accuracy and simple and convenient to operate.