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New tigecycline crystal form and preparation method thereof

A technology for tigecycline and crystal forms, which is applied in the field of pharmaceutical crystal forms and crystal form preparations, and can solve problems such as complicated process operations and difficulty in large-scale production

Inactive Publication Date: 2013-03-06
BEIJING HOPE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, in the existing tigecycline crystallization method, there are still problems such as complicated process operation and difficulty in realizing large-scale production.

Method used

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  • New tigecycline crystal form and preparation method thereof
  • New tigecycline crystal form and preparation method thereof
  • New tigecycline crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Take 1.0 g of tigecycline, add 12 ml of a mixed solvent (methanol: acetone = 1:1 volume ratio), stir slowly, heat up to 30 ° C, all solids are dissolved, continue stirring for 1 hour, and slowly cool down to -5 ~ 5 ° C, Stirring was continued for 1 to 3 hours, a solid was precipitated, filtered, and dried under reduced pressure to obtain 0.88 g of tigecycline in the crystal form of the present invention, with a yield of 88%.

Embodiment 2

[0032] Take 1.0 g of tigecycline, add 28 ml of a mixed solvent (methanol: acetone = 2:8 volume ratio), stir slowly, raise the temperature to 35 ° C, slowly cool down to -15 ~ 5 ° C, continue stirring for 1 to 3 hours, and a solid precipitates , filtered, and dried under reduced pressure to obtain 0.8 g of tigecycline in the crystal form of the present invention, with a yield of 80%.

Embodiment 3

[0034] Take 1.0 g of tigecycline, add 22 ml of mixed solvent (methanol: acetone = 8: 2 volume ratio), stir slowly, heat up to 35 ° C, all solids dissolve, slowly cool down to 0 ~ 10 ° C, precipitate solids, filter, reduce Press and dry to obtain 0.78 g of tigecycline in the crystal form of the present invention, with a yield of 78%.

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Abstract

The invention relates to a new tigecycline crystal form and a preparation method thereof. The new tigecycline crystal form hardly contains any organic solvent. The preparation method is simple, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical crystal forms and preparation of crystal forms, and in particular relates to a new crystal form of tigecycline and a preparation method thereof. Background technique [0002] Tigecycline (Tigecycline), chemical name: (4S, 4aS, 5aR, 12aS)-9-[2-(tert-butylamino)acetamido]-4,7-bis(dimethylamino)-1,4, 4a, 5, 5a, 6, 11, 12a-octahydro-3, 10, 12, 12a-tetrahydroxy-1, 11-dioxo-2-tetracenecarboxamide, the structural formula is shown in the following formula (I) . Tigecycline is a new broad-spectrum active intravenous antibiotic, which is also active against drug-resistant methicillin-resistant Staphylococcus aureus. Skin and soft tissue infection and complicated intra-abdominal infection in adults, including complicated appendicitis, burn infection, intra-abdominal abscess, deep soft tissue infection and ulcer infection. [0003] [0004] Formula (I) [0005] Tigecycline was first disclosed in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C237/26C07C231/24
Inventor 吴涛于富强刘艳玲刘长茹
Owner BEIJING HOPE PHARMA
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