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Preparation method for vilazodone hydrochloride crystal form XI

A technology of vilazodone hydrochloride and crystal form, applied in the field of medicinal chemistry, can solve the problems of inability to obtain crystal form XI, difficult preparation of crystal form XI, etc., and achieve the effects of stable reaction and mild reaction conditions

Inactive Publication Date: 2019-03-22
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Since the crystal form XI cannot be obtained by referring to the preparation method of the crystal form XI described in the original research patent, in order to solve this problem, this application provides a method for preparing the crystal form XI of vilazodone hydrochloride, aiming at solving the problem that the crystal form XI is difficult to prepare

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Disperse 5.0 g of vilazodone free base in 165 ml of aqueous methanol with a volume ratio of methanol to water of 10 / 1, heat to reflux, add 7.7 ml of 2N hydrochloric acid to the system under reflux, and adjust the pH to 3~4. Stirring was continued under reflux for 1 hour, cooled to room temperature and stirring was continued for 1 hour, then the precipitated crystals were suction-filtered, air-dried at 40°C to constant weight, and 5.3 g of vilazodone hydrochloride was obtained, which was detected as crystal form XI .

Embodiment 2

[0021] Disperse 5.0g of vilazodone free base in 100ml of methanol, add 5.7ml of 2N hydrochloric acid dropwise at room temperature, adjust the pH to 3~4, stir at 15°C±5°C for 4h, and then filter the precipitated crystals with suction , collected the filter cake, and blast-dried to constant weight to obtain 5.4 g of vilazodone hydrochloride, which was detected as crystal form XI.

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Abstract

The invention provides a preparation route for a vilazodone hydrochloride crystal form XI: vilazodone hydrochloride with the crystal form XI is obtained by a series of operations such as dilution, pHregulation, crystallization and drying, and the problem that the crystal form XI cannot be obtained by the route of the prior patent. The drug is used for treating or preventing depression, anxiety, bipolar disorder, mania, dementia, mental disorders associated with psychoactive substances, sexual dysfunction, eating disorder, obesity, fibromyalgia, sleep disorder, psychosis-like mental disorders,cerebral infarction, tension, side effects in hypertension treatment, brain diseases, chronic pain, acromegaly, hypogonadism, secondary amenorrhea and premenstrual syndrome.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a preparation method of antidepressant vilazodone hydrochloride crystal form XI. Background technique [0002] Vilazodone hydrochloride (Vilazodone), chemical name: 5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]-1-piperazinyl]-2-benzo Furocarboxamide hydrochloride, for the treatment of major depressive disorder in adults. The application provides pharmaceutical crystal form XI that can be used for the treatment or prevention of depression, anxiety, bipolar disorder, mania, dementia and mental disorders related to psychoactive substances, sexual dysfunction, eating disorders, obesity, fibromyalgia, sleep disorders disorders, psychotic-like mental disorders, cerebral infarction, tension, side effects of hypertension treatment, brain tonic disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome. Contents of the invention [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12
CPCC07B2200/13C07D405/12
Inventor 贾艳红赵云萍赵国磊
Owner BEIJING VENTUREPHARM BIOTECH
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