NEW CRYSTAL FORMS OF DAPAGLIFLOZIN AND PREPARATION METHOD THEREOF

Title:

NEW CRYSTAL FORMS OF DAPAGLIFLOZIN AND PREPARATION METHOD THEREOF

Document Type and Number:

WIPO Patent Application WO/2020/187150

Kind Code:

A1

Abstract:

Disclosed are new crystal forms of dapagliflozin and a preparation method thereof. Particularly, the X-ray powder diffraction pattern of the crystal form A of dapagliflozin has characteristic diffraction peaks at the following 2θ angles: 6.3±0.2°, 12.5±0.2°, 16.0±0.2°, 18.8±0.2°, 26.4±0.2°, and 27.1±0.2°. The X-ray powder diffraction pattern of the crystal form B of dapagliflozin has characteristic diffraction peaks at the following 2θ angles: 6.3±0.2°, 7.2±0.2°, 14.5±0.2°, 19.6±0.2°, 21.3±0.2°, and 23.6±0.2°. The crystal form A is hemi-ethanol solvate, which is stable when it is baked at 10-30℃. The ethanol solvent can be easily removed by baking at 45-55℃ to obtain the anhydrous crystal form B. The crystal form A is an intermediate state crystal form of the anhydrous crystal form B. At the same time, the crystal form A of hemi-ethanol solvate can be directly used in preparation by performing wet granulation and removing the solvent by baking, and can meet the quality requirements of the preparation. The crystal form B has a low water content, a high purity, a good product stability at 60℃ high temperature, a simple preparation process with mild operation conditions, and is suitable for large scale industrial production.

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Inventors:

GE SHUWANG (CN)
HUANG JITING (CN)
TANG WEI (CN)
YANG WENQIAN (CN)
WANG TIE-LIN (CN)

Application Number:

PCT/CN2020/079204

Publication Date:

September 24, 2020

Filing Date:

March 13, 2020

Export Citation:

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Assignee:

LUOXIN PHARMACEUTICAL SHANGHAI CO LTD (CN)
SHANDONG LUOXIN PHARMACY STOCK (CN)

International Classes:

C07D309/10; A61K31/351; A61P3/10

Domestic Patent References:

WO2016018024A1	2016-02-04
WO2017202264A1	2017-11-30
WO2018029611A1	2018-02-15
WO2016155578A1	2016-10-06
WO2017046730A1	2017-03-23
WO2017118945A1	2017-07-13

Foreign References:

CN107163092A	2017-09-15
CN108084130A	2018-05-29
CN101479287A	2009-07-08

Attorney, Agent or Firm:

SHANGHAI BESHINING LAW OFFICE (CN)

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