Tedizolid ammonium phosphate and its crystal form, preparation method and medical application

A technology of tedizolid ammonium phosphate and crystal form, which is applied in the field of chemical pharmaceuticals, and can solve problems such as unfavorable filtration and drying, unsatisfactory removal of impurities, and small particle size.

Active Publication Date: 2019-08-02
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, although the prior art has disclosed tedizolid phosphate and its crystal form, the solubility of tedizolid phosphate and its crystal form is poor, and the reaction crystallization method is usually used to remove impurities, and its impurity removal effect is not ideal. Small, not conducive to filtration and drying, and its clarity is not easy to meet the standard

Method used

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  • Tedizolid ammonium phosphate and its crystal form, preparation method and medical application
  • Tedizolid ammonium phosphate and its crystal form, preparation method and medical application
  • Tedizolid ammonium phosphate and its crystal form, preparation method and medical application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Dissolve 5 g of tedizolid phosphate crude product (HPLC purity>98%) in 22 ml of 2% ammonia solution at room temperature, and the molar ratio of tedizolid phosphate and ammonia water in the ammonia solution is 1:2 to obtain tedizolid phosphate The crude product of tedizolid ammonium salt was 3.8g, and the obtained tedizolid ammonium phosphate was easy to filter, not agglomerated, and easy to dry.

[0069] ESI-MS 448.89[M-H] - ;

[0070] 1 HNMR (DMSO, 400MHz) δ: 8.92(s, 1H), 8.20(m, 2H), 7.73(m, 2H), 7.52(d, 1H), 7.26(br s, 5H), 4.90(m, 1H) , 4.48(s, 3H), 4.17(t, 1H), 3.99(t, 1H), 3.94(m, 2H).

Embodiment 2

[0072] Dissolve 5 g of tedizolid phosphate crude product (HPLC purity>98%) in 220 ml of 0.1% ammonia solution at room temperature, and the molar ratio of tedizolid phosphate and ammonia water in the ammonia solution is 1:1 to obtain tedizolid phosphate The crude product of tedizolid ammonium salt is 3.2 g, and the obtained tedizolid ammonium phosphate is easy to filter, does not agglomerate, and is easy to dry.

[0073] ESI-MS 448.89[M-H] - ;

[0074] 1 HNMR (DMSO, 400MHz) δ: 8.92(s, 1H), 8.20(m, 2H), 7.73(m, 2H), 7.52(d, 1H), 7.26(br s, 5H), 4.90(m, 1H) , 4.48(s, 3H), 4.17(t, 1H), 3.99(t, 1H), 3.94(m, 2H).

Embodiment 3

[0076]5 g of tedizolid phosphate crude product (HPLC purity>98%) was dissolved in 11 ml of 18% ammonia solution at room temperature, and the molar ratio of tedizolid phosphate and ammonia water in the ammonia solution was 1:9 to obtain tedizolid phosphate The crude product of tedizolid ammonium salt was 4.3g, and the obtained tedizolid ammonium phosphate was easy to filter, not agglomerated, and easy to dry.

[0077] ESI-MS 448.89[M-H] - ;

[0078] 1 HNMR (DMSO, 400MHz) δ: 8.92(s, 1H), 8.20(m, 2H), 7.73(m, 2H), 7.52(d, 1H), 7.26(br s, 5H), 4.90(m, 1H) , 4.48(s, 3H), 4.17(t, 1H), 3.99(t, 1H), 3.94(m, 2H).

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Abstract

The invention relates to ammonium tedizolid phosphate, ammonium tedizolid phosphate crystal and their preparation method and medical use. The preparation method has simple processes and is conducive to industrial production. The ammonium tedizolid phosphate crystal A has good solubility. The preparation method has simple processes, is easy to operate, produces small pollution and can be industrialized. The ammonium tedizolid phosphate crystal drug has high purity, excellent physical and chemical properties, good chemical stability and reproducibility of processing. Compared with the tedizolid phosphate crystal, the ammonium tedizolid phosphate crystal A has good solubility, good clarity, a fast filtration rate, good hygroscopicity and good color.

Description

technical field [0001] The present invention relates to the field of chemical pharmacy, more specifically, the present invention relates to tedizolid ammonium phosphate and its crystal form, preparation method of tedizolid ammonium phosphate and its crystal form, and tedizolid ammonium phosphate and the medical application of its crystal form. [0002] technical background [0003] Tedizolid Phosphate is a new oxazolidinone antibiotic developed by Cubist Pharmaceuticals, which was approved by the US FDA on June 20, 2014. For the treatment of acute bacterial skin and skin tissue infections in adults caused by Gram-positive bacteria such as Staphylococcus aureus (including methicillin-resistant strains and methicillin-sensitive strains), various streptococci and enterococci. This is the second new antibiotic drug approved by the FDA for the treatment of ABSSSI infection following the approval of dalbavancin on May 23. Domestically, Bayer Pharmaceuticals and Healthcare Co., Lt...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/6558A61K31/675A61P31/04A61P17/00A61P11/00A61P1/00A61P13/02A61P9/00A61P19/00A61P19/02
CPCC07B2200/13C07F9/65583
Inventor 李娜张亮施珍娟赵敏陈小虎
Owner ZHEJIANG HISUN PHARMA CO LTD
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