New crystal forms of trelagliptin, and preparation methods and application of crystal forms

A technology of crystal forms and uses, applied in the field of organic chemistry, can solve problems such as undisclosed solid forms

Inactive Publication Date: 2016-04-27
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] CN1926128A, CN101360723A etc. disclose the preparation method of Trexagliptin, but all do not disclose its solid form

Method used

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  • New crystal forms of trelagliptin, and preparation methods and application of crystal forms
  • New crystal forms of trelagliptin, and preparation methods and application of crystal forms
  • New crystal forms of trelagliptin, and preparation methods and application of crystal forms

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] The preparation of embodiment 1 Trexagliptin crystal form F

[0101] Dissolve 7.0g of trexagliptin in 30ml of 1,2-propanediol at 95-100°C, stir and dissolve, cool to room temperature and let stand overnight, filter with suction, beat the filter cake with 20ml of ethyl acetate for about 0.5 hours Trexagliptin crystal form F was obtained.

[0102] The measured powder X-ray diffraction pattern is shown in figure 1 , its measured value is as follows (get the measured value corresponding to the diffraction peak whose relative intensity is greater than 1%):

[0103]

[0104]

Embodiment 2

[0105] The preparation of embodiment 2 Trexagliptin crystal form F

[0106] At 80-90°C, dissolve 2.0g of trexagliptin in a mixed solvent of 2.5ml of 1,2-propanediol and 2.5ml of ethyl acetate, stir and dissolve, cool to room temperature naturally, and filter with suction to obtain trexagliptin crystals Type F.

Embodiment 3

[0107] The preparation of embodiment 3 Trexagliptin crystal form F

[0108] At 80-90°C, dissolve 6.0g of Trexagliptin in a mixed solvent of 4ml of 1,2-propanediol and 8ml of ethyl acetate, stir and dissolve, cool to room temperature naturally, filter with suction, and beat the filter cake with 30ml of ethyl acetate After about 1 hour, dry under reduced pressure at 30-40° C. to obtain trexagliptin crystal form F.

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PUM

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Abstract

The invention relates to new crystal forms of trelagliptin, and preparation methods and application of the crystal forms. Specifically, the invention relates to two new crystal forms of trelagliptin as a dipeptidyl peptidase IV inhibitor and preparation methods of the two new crystal forms, a pharmaceutical composition containing the new crystal forms of trelagliptin, and application of the new crystal forms of trelagliptin in manufacturing drugs for treating dipeptidyl-peptidase-IV-mediated diseases.

Description

technical field [0001] The present invention relates to the fields of organic chemistry and pharmacy, in particular to new crystal forms of Trexagliptin and their preparation methods and uses, pharmaceutical compositions containing these new crystal forms, and the use of these new crystal forms for the preparation of dipeptide-based Use in medicine for peptidase IV (DPP-IV) mediated diseases. Background technique [0002] Trelagliptin, chemical name: 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4- Dioxy-1(2H)-pyrimidinyl]methyl]-4-fluoro-benzonitrile, the structure is shown in formula I: [0003] [0004] Trexagliptin is an inhibitor of dipeptidyl peptidase IV (DPP-IV), a serine amino dipeptidase that removes XFF-Pro from the amino terminus (N-terminus) of polypeptides and proteins dipeptide. DPP-IV is constitutively expressed on epithelial and endothelial cells of a variety of different tissues (gut, liver, kidney and placenta), is also found in body flui...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61K31/513A61P3/10A61P3/00A61P3/04A61P1/00A61P29/00A61P17/06A61P19/02A61P35/00
Inventor 胡志鹏林志忠付李袁道义徐同利周仕川李方群罗杰向志祥
Owner SICHUAN HAISCO PHARMA CO LTD
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