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Method for preparing bupropion hydrobromid crystal I

A technology of bupropion hydrobromide, crystal form, applied in the preparation of organic compounds, chemical instruments and methods, organic chemistry and other directions, can solve the influence of preparation stability, poor thermodynamic stability, bupropion hydrobromide Impure crystal form and other problems, to achieve the effect of simple operation and low environmental protection pressure

Active Publication Date: 2014-01-08
ZHEJIANG APELOA JIAYUAN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Since the thermodynamic stability of bupropion hydrobromide crystal form I is slightly worse than that of crystal form II, part of bupropion hydrobromide crystal form I changes into crystal form II after a long period of storage, resulting in the formation of amphetamine hydrobromide The crystal form of hexaketone is impure, which has a certain impact on the stability of the preparation

Method used

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  • Method for preparing bupropion hydrobromid crystal I
  • Method for preparing bupropion hydrobromid crystal I

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Take 50g of bupropion hydrobromide crystal form II, put it into a 250mL three-necked round bottom flask, stir and heat at -0.08MPa, raise the temperature to 170-180°C, keep it warm for 4 hours, cool to room temperature, and detect by PXRD, hydrogen The crystalline form II of bupropion bromide was completely transformed into the crystalline form I.

Embodiment 2

[0021] Put 5g of the mixture of bupropion hydrobromide crystal form II and crystal form I in a watch glass, heat in an oven at 150-160°C for 6 hours, cool to room temperature, and detect by PXRD, amphetamine hydrobromide The ketone form II was completely transformed into form I.

Embodiment 3

[0023] Put 5g of bupropion hydrobromide crystal form II into a 25mL three-necked flask, stir and heat up to 190-200°C for 1 hour under airtight conditions, cool to room temperature, and detect by PXRD, bupropion hydrobromide Form II is all converted to Form I.

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Abstract

The invention relates to a method for preparing bupropion hydrobromid crystal I, which comprises: heating bupropion hydrobromid crystal I or mixture of the bupropion hydrobromid crystal I and bupropion hydrobromid crystal II, of which the chemical purity is qualified, to 150 to 210 DEG C, keeping the temperature at 150 to 210 DEG C for 0.5 to 10 hours, and cooling to room temperature to the bupropion hydrobromid crystal I which is the target product. According to the result of powder X-ray diffraction (PXRD) detection, the target product does not have the characteristic peak of the bupropion hydrobromid crystal II; and an initiative raw material is converted into the bupropion hydrobromid crystal I completely. The result of high performance liquid chromatography (HPLC) detection indicates that new impurities are not produced and that the impurity content does not change. The method has the advantages of simple and convenient operation, suitability for industrial mass production, small environment-protection pressure and the like.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical manufacturing, in particular to a preparation method of bupropion hydrobromide crystal form I. Background technique [0002] Bupropion Hydrobromide is an antidepressant drug with the following structural formula: [0003] [0004] There are several crystal forms of bupropion hydrobromide. U.S. Patent No. US7553992 discloses three crystal forms of bupropion hydrobromide: polymorph I, II and III, wherein, crystal forms I and II are relatively stable solvent-free crystal forms, and crystal form III is ethanol Solvates are slightly less stable. [0005] Chinese patent document CN101811975A discloses crystal form IV and crystal form V. Crystal form IV is a stable solvent-free crystal form, and crystal form V is n-propanol solvate, which is more stable than crystal form III disclosed in patent document US7553992. [0006] Patent document WO2010015692A2 discloses additional bupropion hydrobr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C225/16C07C221/00
Inventor 皋海涛张国庆张拥军吴瑜亮王海涛吴琳琳茅晔
Owner ZHEJIANG APELOA JIAYUAN PHARMA