Novel method for preparing amorphous Ivabradine hydrochloride

An ivabradine hydrochloride and amorphous technology, which is applied in the field of preparation of amorphous ivabradine hydrochloride, can solve the problems of low production efficiency and achieve the effects of improving production efficiency, high yield and high content

Active Publication Date: 2011-05-11
YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA +1
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  • Abstract
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  • Application Information

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Problems solved by technology

[0009] The purpose of the present invention is to provide a new method for preparing amorphous ivabradine hydrochloride for the low production efficiency problem in the preparation method of amorphous ivabradine

Method used

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  • Novel method for preparing amorphous Ivabradine hydrochloride
  • Novel method for preparing amorphous Ivabradine hydrochloride

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Experimental program
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Effect test

Embodiment 1

[0022] 100g of ivabradine hydrochloride is added in 1000ml of ethanol, stirred to dissolve. The resulting solution was added into 4000ml of ether to obtain a mixed solution, which was stirred at a high speed at 15°C-30°C. The resulting crystalline slurry was stirred for 1 hour. The crystalline slurry was cooled to about 0° C., stirred for 2 hours, filtered, and dried to collect 81 g of amorphous ivabradine hydrochloride with a yield of 81.0%.

[0023] The powder X-ray diffraction pattern of amorphous ivabradine hydrochloride is shown in the attached Figure 1 .

Embodiment 2

[0025] 100g of ivabradine hydrochloride is added in 1000ml of acetone, stirred to dissolve. The resulting solution was added into 3000ml of cyclohexane to obtain a mixed solution, which was stirred at a high speed at 15°C-30°C. The resulting crystalline slurry was stirred for 1 hour. The crystalline slurry was cooled to about 0° C., stirred for 2 hours, filtered, and dried to collect 83 g of amorphous ivabradine hydrochloride with a yield of 83.0%.

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Abstract

The invention provides a novel method for preparing amorphous Ivabradine hydrochloride, which comprises the following steps: firstly, Ivabradine hydrochloride is dissolved in a solvent to form a solution, and secondly, the solution is added into a non-solvent, a mixed solution is obtained through stirring, and amorphous Ivabradine hydrochloride is obtained after cooling. The method has the advantage that the traditional two-step amorphous preparation method (crystal type high-quality product is produced at first and then amorphous is prepared through a concentration method) is integrated into one step, so as to achieve high yield and greatly improve the production efficiency.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular, the invention relates to a preparation method of amorphous ivabradine hydrochloride. Background technique [0002] Ivabradine hydrochloride, its chemical name is 3-[3-[[(8S)-3,4-dimethoxy-8-bicyclo[4.2.0]oct-1,3,5-triene]methanol Base-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepine-4-one hydrochloride, the structural formula is as follows [0003] [0004] Ivabradine hydrochloride is an If inhibitor for the treatment of chronic stable angina symptoms in patients with normal sinus rhythm who are contraindicated or intolerant to beta-blockers. [0005] Many patents disclose ivabradine hydrochloride, its preparation method and the preparation of key intermediates. These patents include: EP534859, US5296482, FR19910011894, CN1699331A, CN1683342A, CN1683343A, CN1683341A. [0006] In addition, many patents disclose methods for polymorphic forms of ivabradine h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D223/16
Inventor 张培龙石和鹏侯鹏林卓李玉宽宋志涛周津梅
Owner YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA
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