A crystal form of urat1 inhibitor and its preparation method

A technology of crystal form and map, applied in the field of crystal form and preparation of URAT1 inhibitor, can solve the problem that the additional effect is not very significant and so on

Active Publication Date: 2022-04-19
DONGBAO PURPLE STAR (HANGZHOU) BIOPHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Approved its 200mg dose combined with xanthine oxidase inhibitor XOI (such as Febuxostat, etc.) for the treatment of hyperuricemia and gouty arthritis, but compared with xanthine oxidase inhibitor alone, the additional The effect is not very significant

Method used

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  • A crystal form of urat1 inhibitor and its preparation method
  • A crystal form of urat1 inhibitor and its preparation method
  • A crystal form of urat1 inhibitor and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Embodiment 1: the preparation of formula (I) compound

[0070]

[0071] synthetic route:

[0072]

[0073] Step 1: Synthesis of Compound 2

[0074] Add 4.5 L of dimethyl sulfoxide to a three-neck flask (10 L), add potassium tert-butoxide (836.66 g, 7.46 mol, 2 eq) under stirring, and continue stirring for 10 minutes until the solution is clear, and then cool to The internal temperature of the reaction solution is 20-25°C. Add compound 1 (500.05g, 3.73mol, 1eq) dimethyl sulfoxide (500mL) solution dropwise to the above solution, after dropping, stir and react for 30 minutes, then add carbon disulfide (283.86g, 3.73mol, 1eq ), dropwise, continued stirring reaction for 30 minutes. Ethyl bromoacetate (1250 g, 7.46 mol, 2 eq) was added dropwise thereto, and the reaction was continued to stir for 2 hours after the drop was completed. Finally, potassium carbonate (515.52 g, 7.46 mol, 1 eq) was added, and the temperature was raised to 65° C. to continue stirring for 8 ...

Embodiment 2

[0098] Embodiment 2: Preparation of the A crystal form of the compound of formula (I)

[0099] Add the compound of formula (I) (50mg) into a glass bottle, add methanol (0.4mL) respectively, and stir to form a suspension or solution. The above suspension sample was placed in a constant temperature mixer (40° C.), shaken at 40° C. for 60 hours, and then centrifuged to collect the sample. The above dissolved samples were volatilized at room temperature and then centrifuged to collect the samples. The above sample was dried overnight in a vacuum drying oven (40° C.), and its crystal form was detected by XRPD, and the crystal form of the final product obtained was Form A of the compound of formula (I).

[0100]Add the compound of formula (I) (50mg) into a glass bottle, add ethyl acetate (0.4mL) respectively, and stir to form a suspension or solution. The above suspension sample was placed in a constant temperature mixer (40° C.), shaken at 40° C. for 60 hours, and then centrifuge...

Embodiment 3

[0101] Embodiment 3: Preparation of the B crystal form of the compound of formula (I)

[0102] Add the compound of formula (I) (50 mg) into a glass bottle, add tetrahydrofuran (0.4 mL), and stir until it dissolves. The above dissolved samples were volatilized at room temperature and then centrifuged to collect the samples. The collected samples were dried overnight in a vacuum drying oven (40° C.), and the crystal form state was detected by XRPD. The crystal form of the final product obtained was Form B of the compound of formula (I).

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Abstract

The invention discloses a crystal form of URAT1 inhibitor and a preparation method thereof.

Description

[0001] Cross References to Related Applications [0002] CN201711181960.2, application date 2017.11.23. technical field [0003] The invention relates to a crystal form of URAT1 inhibitor and a preparation method thereof. Background technique [0004] Uric acid is a product of the metabolism of purine compounds in animals. For humans, due to the lack of uricase that can continue to oxidize and degrade uric acid in the human body, uric acid is excreted in the human body as the final product of purine metabolism through the intestines and kidneys, and renal excretion is the main way for uric acid excretion in the human body. The upper limit of the normal uric acid concentration range in the human body is: 400 μmol / L (6.8 mg / dL) for men and 360 μmol / L (6 mg / dL) for women. Abnormal uric acid levels in the human body are often due to increased uric acid production or decreased uric acid excretion. Diseases related to abnormal uric acid levels include hyperuricemia, gout, etc. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D409/04A61K31/4196A61P19/06
CPCA61K31/4196A61P19/06C07D409/04C07B2200/13
Inventor 王建非张杨朱文元黎健陈曙辉
Owner DONGBAO PURPLE STAR (HANGZHOU) BIOPHARMACEUTICAL CO LTD
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