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Polymorphic substance of guanfacine hydrochloride and preparation method thereof

A kind of technology of guanfacine hydrochloride and crystal form, which is applied in the polymorphic form of guanfacine hydrochloride and the field of preparation thereof, and can solve the problems of unseen crystal form, reports and the like

Inactive Publication Date: 2013-03-27
BEIJING D VENTUREPHARM TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] At present, there are many literature reports on the synthesis of guanfacine hydrochloride, but there is no report on its crystal form

Method used

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  • Polymorphic substance of guanfacine hydrochloride and preparation method thereof
  • Polymorphic substance of guanfacine hydrochloride and preparation method thereof
  • Polymorphic substance of guanfacine hydrochloride and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1: the preparation method of guanfacine hydrochloride crystal form A

[0017] Add 10.0g of guanfacine hydrochloride sample qualified for related substances into a 100ml three-necked round-bottomed flask, then add 35ml of acetonitrile and 5ml of drinking water in sequence, start magnetic stirring and heating with a heating mantle, and heat to 50°C to completely dissolve the guanfacine hydrochloride sample , continued heating to 67°C and began to reflux, then stopped heating, and naturally cooled to room temperature (10°C) without removing the heating mantle, a needle-shaped white solid was precipitated, and dried by air at 45°C to obtain 6.2 g of the product, with a yield of 62%. The melting point is 203.6°C-206.0°C. Differential scanning calorimetry (DSC) data ( figure 2 ) and X-ray powder diffraction data ( figure 1 ) proved to be Form A.

Embodiment 2

[0018] Embodiment 2: the preparation method of guanfacine hydrochloride crystal form A

[0019] Add 3.8g of guanfacine hydrochloride sample qualified for related substances into a 100ml beaker, then add 20ml of tetrahydrofuran, and stir magnetically. At this time, the system is a paste, which is dissolved immediately after adding 3ml of drinking water, and a white solid is precipitated after being left at room temperature for two days. Filtration and blast drying at 45°C gave 3.3 g of the product with a melting point of 203.6°C-205.8°C. Form A was confirmed by differential scanning calorimetry (DSC) data and X-ray powder diffraction data.

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Abstract

The invention belongs to the technical field of medicaments, and in particular relates to a polymorphic substance of guanfacine hydrochloride and a preparation method thereof. The crystal of the guanfacine hydrochloride is obtained by dissolving the guanfacine hydrochloride with a mixed solvent of RCN and water under the reflux heating condition, filtering and drying.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a polymorph of guanfacine hydrochloride and a preparation method thereof. Background technique [0002] The chemical name of guanfacine hydrochloride is N-amidino-2-(2,6-dichlorophenyl)acetamide monohydrochloride, and its structural formula is shown in formula (I). The original researcher is SHIRE company in the UK. Guanfacine hydrochloride is currently approved by the FDA. Its therapeutic areas include attention deficit hyperactivity disorder (ADHD), and may also be used to treat mild to moderate high blood pressure, heroin withdrawal symptoms, certain problems in pregnancy difficulties, sleep disturbances, and more. Pilot studies for other indications are currently underway. This medicine is especially useful for children who have both ADHD and a behavioral disorder. [0003] [0004] At present, there are many literature reports on the synthesis...

Claims

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Application Information

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IPC IPC(8): C07C279/22C07C277/08
Inventor 王进敏郭夏宋雪梅
Owner BEIJING D VENTUREPHARM TECH DEV
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