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Canagliflozin anhydrous compound

A technology of hydrates and compositions, 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 anhydrous compound
  • Canagliflozin anhydrous compound
  • Canagliflozin anhydrous compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] In a 500ml reaction bottle equipped with stirring, thermometer and condenser, add 60 grams of canagliflozin and 300 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.

[0043] Cool 1150ml of acetonitrile-methyl ethyl ketone = 5:5 mixture to 13°C, add the above standby solution while stirring, keep warm for 18 hours, crystals precipitate, filter, and dry to obtain 54.4 grams of white crystals. Purity 99.9% (HPLC normalization method), optical purity 99.96% ee (chiral HPLC).

[0044] Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa, 40Kv, 100mA; 2θ scanning range: 0-50 ° .

[0045]

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Abstract

The invention belongs to the technical field of medicine, and in particular to a Canagliflozin anhydrous crystal form and a preparation method thereof. The Canagliflozin prepared by the invention has the advantages of chemical purity of 99.9%, maximum is less than 1 per thousand, optical purity of up to 99.96% ee and good stability. The invention also relates to application of the crystal form composition to preparation of medicaments for 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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