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Tigecycline and preparation method thereof

A technology of tigecycline and hydrochloride, which is applied to the preparation of carboxylic acid amides, chemical instruments and methods, and the preparation of organic compounds, etc., to achieve the effect of wide application prospects

Inactive Publication Date: 2009-03-18
SHANGHAI LAIYI BIOMEDICAL RES & DEV CENT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the various salts of tigecycline have not been reported yet

Method used

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  • Tigecycline and preparation method thereof
  • Tigecycline and preparation method thereof
  • Tigecycline and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1 , Preparation of various acid aqueous solutions

[0015] Preparation of hydrochloric acid aqueous solution: measure 0.8 mL concentrated hydrochloric acid (analytical pure, HCl content 36.0-38.0%), add water to make up to 10 mL.

[0016] Preparation of acetic acid aqueous solution: weigh 0.6g of glacial acetic acid, add water to make up to 10mL.

[0017] Preparation of methanesulfonic acid aqueous solution: Weigh 1.0 g of methanesulfonic acid (analytical pure, content 98%), add water to make up to 10 mL.

[0018] Preparation of aqueous solution of benzenesulfonic acid: weigh 1.6 g of benzenesulfonic acid (analytical pure, content 70%), add water to make up to 10 mL.

[0019] Preparation of lactic acid aqueous solution: Weigh 0.9 g of natural lactic acid (analytical pure, content 99%), add water to make up to 10 mL.

Embodiment 2

[0020] Example 2 , the preparation of tigecycline hydrochloride

[0021] Weigh 0.3 g of tigecycline, dissolve it in 15 mL of water, add 0.5 mL of the hydrochloric acid aqueous solution obtained in Example 1, stir fully to make the two react completely, and the specific reaction formula is as follows:

[0022]

[0023] The reaction solution was frozen in a refrigerator at -20° C. for 5 hours, and then freeze-dried in a lyophilizer overnight to obtain tigecycline hydrochloride powder.

Embodiment 3

[0024] Example 3 , the preparation of tigecycline acetate

[0025] Weigh 0.3g of tigecycline, dissolve in 15mL of water, add 0.5mL of the aqueous acetic acid obtained in Example 1, fully stir to make the two react completely, and the specific reaction formula is as follows:

[0026]

[0027] The reaction solution was frozen in a refrigerator at -20° C. for 5 hours, and then freeze-dried in a freeze dryer overnight to obtain tigecycline acetate powder.

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PUM

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Abstract

The present invention provides tigecycline and a method for preparing tigecycline salt. The tigecycline salt is obtained through the reaction of tigecycline and a corresponding acid. The tigecycline salt is apparently better in water-solubility and bacteriostasis activity, compared with the tigecycline in a dissociative state, and thus the method has a wide application prospect.

Description

technical field [0001] The invention belongs to the field of chemical industry and pharmacy, and in particular relates to a tigecycline salt and a preparation method thereof. Background technique [0002] Tigecycline (tigecycline), chemical name: (4S, 4aS, 5aR, 12aS)-4,7-bis(dimethylamino)-9-[(tert-butylamino)acetamido]-3,10, 12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide, also known as 9-tert-butylglycerol Aminoamido minocycline or Dingglyminocycline, which was approved by the FDA in June 2005, is the first glycylcycline antibiotic approved for marketing. The molecular structure is as follows: [0003] [0004] Although tigecycline and minocycline have many similarities in structure, the former is obviously superior to traditional tetracyclines in terms of antibacterial spectrum range and drug-resistant bacteria, and has broad-spectrum antimicrobial activity. Treatment of complicated intra-abdominal infections (cIAI) and complicate...

Claims

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Application Information

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IPC IPC(8): C07C237/26C07C231/12
Inventor 邵昌王涛杨志钧袁建勇陈鹏叶伟东罗敏玉戈梅
Owner SHANGHAI LAIYI BIOMEDICAL RES & DEV CENT
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