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R-lansoprazole crystal form and preparation method therefor

A technology of lansoprazole crystals and crystal forms, which is applied in the field of chemical synthesis of dexlansoprazole crystal forms and its preparation, can solve the problems of poor stability of dexlansoprazole, low stability of preparation products, sensitivity to humidity, etc. problems, to achieve better physical and chemical properties, mild conditions, and high stability

Inactive Publication Date: 2015-11-04
HEFEI ANDERSON PHARMA CO LTD
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Problems solved by technology

[0011] For the deficiencies in the prior art, for existing dexlansoprazole poor stability, sensitive to humidity, difficult to operate in the preparation process, high production cost, and the defects of low stability of the preparation product, and provide a kind of Anhydrous dexlansoprazole crystal form and preparation method thereof, the new dexlansoprazole crystal form has better physical and chemical properties, high melting point and better stability, and is suitable for use in pharmaceuticals

Method used

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  • R-lansoprazole crystal form and preparation method therefor
  • R-lansoprazole crystal form and preparation method therefor
  • R-lansoprazole crystal form and preparation method therefor

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Embodiment Construction

[0026] In order to make the purpose, technical solutions and advantages of the embodiments of the present invention more clear, the technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention and the drawings of the embodiments. Obviously, the described implementation Examples are some embodiments of the present invention, not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without creative efforts fall within the protection scope of the present invention.

[0027] Dexlansoprazole can be prepared using the preparation method of the reference literature Chemical and Bioengineering, 2014(31):1672-5425.

[0028] One, the preparation of dexlansoprazole crystal form

[0029] S1: Synthesis of 2-{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridine]methylthio}benzimidazole

[0030] Add 88.0g...

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Abstract

The invention provides an R-lansoprazole crystal form and a preparation method therefor and relates to the field of medicinal chemical industry. 2[theta] values of characteristic peaks of an X-ray powder diffractogram of the R-lansoprazole crystal form are 6.01, 6.82, 8.80, 12.23, 13.33, 14.54, 17.96, 18.86, 19.91, 20.32, 20.75, 22.10, 23.08, 23.75, 26.09, 29.68 and 32.45. The preparation method for the R-lansoprazole crystal form provided by the invention is simple and is mild in conditions and stable and controllable in preparation process; and shown by stability research, the crystal form product prepared by the method has better physicochemical properties and higher stability, is suitable for being applied to pharmaceuticals and can be used for preventing and treating gastric acid related diseases when the product is applied to pharmaceutical compositions.

Description

technical field [0001] The invention relates to the field of medicine and chemical industry, in particular to the chemical synthesis of dexlansoprazole crystal form and its preparation method. Background technique [0002] Lansoprazole, chemical name: 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]-sulfinyl ]-1H-benzimidazole, molecular formula C16H14F3N3O2S, molecular weight 369.36. It was successfully developed by Takeda Corporation of Japan, and then launched in France, Japan, and the United States successively. It is the second proton pump inhibitor to be marketed after omeprazole. Lansoprazole is a drug that inhibits gastric acid secretion and is mainly used in the treatment of gastric ulcer, duodenal ulcer, anastomotic ulcer, Helicobacter pylori infection, reflux esophagitis, gastrinoma and other diseases. Has higher bioavailability and fewer side effects. Unlike racemic lansoprazole, the amorphous form of dexlansoprazole is not stable enough, so a lot of ...

Claims

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Application Information

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IPC IPC(8): C07D401/12
CPCC07D401/12C07B2200/13
Inventor 任磊宋威
Owner HEFEI ANDERSON PHARMA CO LTD
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