63 results about "Vilazodone" patented technology

The invention discloses a new method for preparing 3-(4- chlorobutyl)-1H-5-cyanoindole as a vilazodone intermediate, comprising the following steps: step (1), a compound of formula II is reacted with a compound of formula III in the presence of an acylation catalyst in an organic solvent to form a compound of formula IV, step (2), the compound of formula IV formed in step (1) is subjected to carbonyl reduction reaction in the presence of a reducing catalyst in the organic solvent. The preparation method for 3-(4- chlorobutyl)-1H-5-cyanoindole as the vilazodone intermediate has cheap and easily-available raw materials, mild reaction condition, simple operation, high synthesis efficiency and is suitable for industrial production, thereby providing a new way for preparing vilazodone.

The invention provides a method of preparing vilazodone and an intermediate thereof. The method comprises the following steps: obtaining the intermediate shown as a formula (V) through a coupling reaction; and obtaining vilazodone by reducing an acetylenic bond and removing an N protective radical for the intermediate shown as the formula (V); or further converting to obtain vilazodone. The method provided by the invention overcomes the deficiencies in existing preparation of vilazodone and the intermediate thereof. The raw material is easy to obtain, the reaction yield is high, and the method is suitable for industrialized production and has a greater application value.

The present invention provides a synthesis method for an antidepressant drug vilazodone, belonging to the technical field of drug synthesis, and the method comprises the steps of: reacting 5-nitrosalicylaldehyde as a raw material with ethyl bromoacetate under the action of potassium carbonate by heating, to obtain a compound 5-nitrobenzofuran-2-carboxylic acid via hydrolysis; adding in aqueous ammonia after the reaction between 5-nitro-benzofuran-2-carboxylic acid and isobutyl chloroformate is completed, to give 5-nitrobenzofuran-2-carboxamide; reducing the 5-nitrobenzofuran-2-carboxamide by using sodium hydrosulfite to give an intermediate 5-aminobenzofuran-2-carboxamide; cyclizing the 5-aminobenzofuran-2-carboxamide with bis(2-chloroethyl)amine in the action of an alkaline to give 5-piperazinyl-benzofuran-2-carboxamide; and subjecting the 5-piperazinyl-benzofuran-2-carboxamide and 3-(4-chloro-butyl)-5-cyano indole to a substitution reaction to obtain the vilazodone. According to the synthesis method of the invention, the raw materials are cheap, and the reaction process is simple.

The invention discloses a hydrochloric acid vilazodone quick-release tablet and a preparation method thereof. The hydrochloric acid vilazodone quick-release tablet comprises the follow components by mass: 2-12% of hydrochloric acid vilazodone, 28-45% of lactose, 40-60% of microcrystalline cellulose, 0.5-3% of lubricants and 1-5% of coating materials. The lubricants include magnesium stearate and colloidal condition silica or one of the magnesium stearate and the colloidal condition silica. The hydrochloric acid vilazodone quick-release tablet is prepared through the following steps: evenly mixing the hydrochloric acid vilazodone, the lactose, the microcrystalline cellulose and the lubricants according to proportion of a formula, detecting whether content uniformity is qualified, and pressing the mixture into tablets when the content uniformity is qualified. The hydrochloric acid vilazodone quick-release tablet has special requirements for grain size of the hydrochloric acid vilazodone, and the preparation process saves time and labor, reduces energy consumption and improves production efficiency. Disintegration speed of medicines is fastened, the dissolving-out time is obviously less than that of a prescription which has no limitation on the grain size of the hydrochloric acid vilazodone, and simultaneously the process which directly performs mixing tabletting greatly improves stability of the medicines in preparations.

The invention relates to a preparation method of 5-(piperazine-1-group) benzofuran-2-carboxylic acid ethyl ester. 5-(piperazine-1-group) benzofuran-2-carboxylic acid ethyl ester is an important intermediate for synthetizing hydrochloric vilazodone. Under the existence of alkali and phase transfer catalyst, 5-amino-benzofuran-2-carboxylic acid ethyl ester and N, N-di (2-chlorine ethyl) amine hydrochloride are reacted in solvent, reaction time is 2-6 hours, and reaction temperature ranges from room temperature to backflow temperature of the solvent. By the preparation method, reaction time is shortened, and yield rate and purity of products are improved. The preparation method is simple, reliable and low in production cost and has higher implement value and social and economic benefits.

The invention discloses a vilazodone orally disintegrating tablet which has good taste, does not need water for administration, is capable of quickly disintegrating after entering the mouth, suitable for patients, having trouble in swallowing, like old people and psychiatric patients to take and also suitable for administration under conditions that water is difficult to get during travelling and wartime. an indication of the vilazodone orally disintegrating tablet is major depression disorder of adults, and administration compliance of the patients can be improved due to good taste and a simple and quick administration mode. In addition, the invention further discloses a preparation method of the vilazodone orally disintegrating tablet. The preparation method is simple in process and low in cost. The orally disintegrating tablet prepared by the method is quick to disintegrate and act, so that administration discomfort of the patients is reduced.

Disclosed herein are inclusion complexes comprising vilazodone or a pharmaceutically acceptable salt thereof and an inclusion material, compositions and pharmaceutical formulations comprising the inclusion complexes, and methods for preparing the inclusion complexes, compositions or pharmaceutical formulations.

The invention belongs to the technical field of medicine and relates to a substituted piperazine compound and a preparation method for an intermediate of vilazodone. Substituted piperazine phenol is employed as a raw material and is subjected to a hydroformylation reaction, a cyclization reaction and a formylation reaction to obtain 5-(1-piperazine)-benzofuran-2-methanamide of a salt thereof. Finally vilazodone is prepared. The preparation method overcomes defects in a preparation method in the prior art, is simple in operation, is environment-friendly in processes and is free of any expensive catalysts. The intermediate is convenient to separate, is outstanding in yield, is low in cost and is suitable for industrial production.