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Canagliflozin compound

A technology of canagliflozin and hydrate, which is applied in the field of medicine and can solve problems such as crystallization difficulties

Inactive Publication Date: 2015-03-25
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, it is difficult to obtain the crystalline form of the compound of formula (I) from an organic solvent

Method used

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  • Canagliflozin compound
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Examples

Experimental program
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Effect test

Embodiment 1

[0044]In a 500ml reaction bottle equipped with stirring, thermometer and condenser, add 60 grams of canagliflozin and 400 milliliters of water, add 0.5 grams of dimethylformamide (DMF) to the above aqueous solution, stir for 30 minutes, filter, and the filtrate Cool to 12°C and set aside.

[0045] Cool 800ml of acetonitrile-methyl ethyl ketone = 5:5 mixture to 13°C, add the above standby solution while stirring, keep it warm for 18 hours, crystals precipitate, filter, and dry to obtain 53.3 grams of white crystals. Purity 99.9% (HPLC normalization method), optical purity 99.96% ee (chiral HPLC).

[0046] Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa, 40Kv, 100mA; 2θ scanning range: 0-50 ° .

[0047]

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Abstract

Belonging to the field of medical technologies, the invention in particular relates to a canagliflozin anhydrous compound and a preparation method thereof. The canagliflozin obtained by the invention has the advantage of: chemical purity of 99.9%, maximum impurity of less than 1 per thousand, optical purity up to 99.96 enantiomeric excess percentage, and good stability. The invention also relates to application of the anhydrous crystal composition to preparation of drugs treating type 2 diabetes and related diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to anhydrous canagliflozin and a preparation method thereof, and also relates to the application of a composition using the compound in the treatment of diseases such as type 2 diabetes. Background technique [0002] Patent WO2005 / 012326 discloses a group of compounds that are sodium-dependent glucose transporter (SGLT) inhibitors, and the therapeutic use of these compounds for treating diabetes, obesity, diabetic complications, and the like. 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl of formula (I) described in patent WO2005 / 012326 ]benzene: [0003] [0004] In general, for commercial use it is important that the product possess good handling properties. In addition, there is also a need to manufacture the product in pure and crystalline form so that formulations can meet stringent pharmaceutical requirements and specifications. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D409/10A61K31/381A61P3/10
CPCC07D409/10
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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