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Novel preparation method of III crystal-form vilazodone hydrochloride

A technology of vilazodone and vilazodone hydrochloride, applied in the directions of organic chemistry, organic chemistry, etc., can solve problems such as inability to realize industrialized production, and achieve a shortened process time, good reproducibility, and strong operability. Effect

Inactive Publication Date: 2015-05-13
BEIJING SINICA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the vilazodone hydrochloride II crystal form loses solvent slowly in vacuum drying at 100 to 110°C, after 14 days of drying under this condition, there is still 5% tetrahydrofuran remaining, and this method cannot realize industrial production

Method used

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  • Novel preparation method of III crystal-form vilazodone hydrochloride
  • Novel preparation method of III crystal-form vilazodone hydrochloride
  • Novel preparation method of III crystal-form vilazodone hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Dissolve vilazodone (4.41g, 10mmol) in 30mL of tetrahydrofuran, control the temperature at 25°C, slowly add 3mL of 1N HCl, stir for 30 minutes, a white solid precipitates, filter, and vacuum dry at 120°C for 72 hours to obtain hydrochloric acid Vilazodone III crystal form 4.2g, yield 88%.

Embodiment 2

[0024] Dissolve vilazodone (4.41g, 10mmol) in 30mL of tetrahydrofuran, control the temperature at 30°C, slowly add 3mL of 1N HCl, stir for 30 minutes, a white solid precipitates, filter, and vacuum dry at 130°C for 24 hours to obtain hydrochloric acid Vilazodone III crystal form 4.3g, yield 90%.

Embodiment 3

[0026] Dissolve vilazodone (4.41g, 10mmol) in 30mL of tetrahydrofuran, control the temperature at 40°C, slowly add 3mL of 1N HCl, stir for 30 minutes, a white solid precipitates, filter, and vacuum dry at 150°C for 20 hours to obtain hydrochloric acid Vilazodone III crystal form 4.1g, yield 86%.

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Abstract

The invention belongs to the field of pharmaceutical chemistry, and more specifically to a novel preparation of III crystal-form 1-[4-(5-cyanoindole-3-butyl)]-4-(2-carbamoyl-coumarone-5-yl)-piperazine hydrochloride. The preparation method comprises reacting a solvate of hydrochloric acid, vilazodone and tetrahydrofuran at a temperature range of 120-140 DEG C and performing vacuum drying for 12-36 hours. The III crystal-form vilazodone hydrochloride is stable and is convenient to obtain.

Description

Field of invention: [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a 1-[4-(5-cyanindole-3-butyl)-4-(2-carbamoyl-benzofuran-5-yl)-piper A new preparation method of oxazine hydrochloride III crystal form. Background technique: [0002] The chemical name of vilazodone hydroxamide is 1-[4-(5-cyanindole-3-butyl)-4-(2-carbamoyl-benzofuran-5-yl)- Piperazine hydrochloride, the molecular formula is C 26 h 28 CIN 5 o 2 , the molecular weight is 477.9, and the chemical structural formula is as follows: [0003] [0004] Low levels of monoamine neurotransmitters such as central norepinephrine (NE), 5-hydroxytryptamine (5-HT), and dopamine (DA) and their receptor function are considered to be the cause of depression. Vilazodone hydrochloride is a 5-HT reuptake inhibitor and a partial agonist of 5-HTIA. It can rapidly increase the extracellular concentration of 5-HT while stimulating 5-HTIA receptors, and exert a rapid antidepressan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12
CPCC07D405/12C07B2200/13
Inventor 张翔李小培陈赫岩黄少林赵鸿莲许晓椿
Owner BEIJING SINICA TECH
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