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Piperacillin sodium compound containing half water

A technology of piperacillin sodium and compound, which is applied in the field of 1/2 water piperacillin sodium compound and its preparation method, can solve the problems of poor quality and stability, long production cycle, not conforming to the concept of energy saving and consumption reduction, etc.

Inactive Publication Date: 2019-01-04
陈立平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The industrial preparation of piperacillin sodium generally adopts the freeze-drying method, which has a long production cycle, high power consumption, poor quality and stability, and does not meet the current concept of energy saving and consumption reduction.

Method used

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  • Piperacillin sodium compound containing half water
  • Piperacillin sodium compound containing half water
  • Piperacillin sodium compound containing half water

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Preparation of 1 / 2 water piperacillin sodium compound

[0030] 1. Preparation process:

[0031] (1) 100.4 g of ampicillin trihydrate, 200 mL of ethyl acetate and 400 mL of water were added to the reactor, and the reaction was stirred. Triethylamine was added dropwise to adjust the pH to 7.1, the temperature was controlled at 15-20°C, 65.9 g of 4-ethyl-2,3-dioxypiperazinecarbonyl chloride was added, and the reaction was incubated for 1 h. Activated carbon 5.0g was added, decolorized for 30min, and filtered. The aqueous layer in the filtrate was taken, added with an equal volume of ethyl acetate, adjusted to pH 1.6 with 2 mol / L hydrochloric acid, stirred for 2 h, filtered, and vacuum-dried at 30°C for 2.5 h to obtain 123.5 g of piperacillin acid as a white solid.

[0032] (2) Dissolve 123.5 g of the white solid above in a mixed solution of 1000 mL of acetone and 300 mL of water, cool down to 5°C, add 48.7 g of sodium acetate, and keep the temperature for 2 h. ...

Embodiment 2

[0037] Example 2 Preparation of 1 / 2 water piperacillin sodium compound

[0038] 1. Preparation process:

[0039] (1) 100.1 g of ampicillin trihydrate, 200 mL of ethyl acetate and 400 mL of water were added to the reactor, and the reaction was stirred. Triethylamine was added dropwise to adjust the pH to 7.5, the temperature was controlled at 15 to 20° C., 65.7 g of 4-ethyl-2,3-dioxypiperazinecarbonyl chloride was added, and the reaction was incubated for 1 h. Activated carbon 5.0g was added, decolorized for 30min, and filtered. The water layer in the filtrate was taken, added with an equal volume of ethyl acetate, adjusted to pH 1.9 with 2 mol / L hydrochloric acid, stirred for 2 h, filtered, and dried under vacuum at 35°C for 2 h to obtain 121.8 g of piperacillin acid as a white solid.

[0040] (2) 121.8g of above-mentioned white solid was dissolved in a mixed solution of 1050mL of acetone and 350mL of water, cooled to 8°C, 48.0g of sodium acetate was added thereto, and the r...

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Abstract

The invention discloses a piperacillin sodium compound containing half water and a preparation method thereof. Each mole of piperacillin sodium contains a half mole of water. First, ampicillin trihydrate is reacted with 4-ethyl-2,3-dioxypiperazine formyl chloride to form piperacillin acid, then piperacillin acid is reacted with sodium acetate in a mixed solution of acetone and water, isopropanol is added dropwise, and crystallization, filtration and drying are conducted to obtain the piperacillin sodium compound containing half water. The piperacillin sodium compound containing half water hashigh fluidity, low hygroscopicity and impurity content, high thermodynamic stability and a wider application prospect.

Description

technical field [0001] The invention belongs to the technical field of chemical engineering medicine crystallization, and relates to a 1 / 2 water piperacillin sodium compound and a preparation method thereof. Background technique [0002] Piperacillin Sodium is a semi-synthetic broad-spectrum antibiotic of penicillin. Developed by Japan Toyama Chemical Industry Co., Ltd. in 1972, it is mainly used for serious infections caused by Pseudomonas aeruginosa and various sensitive gram-negative bacilli, such as bloodstream infections, lower respiratory tract infections, bone and joint infections, and urinary tract infections. , biliary tract infection, abdominal infection, pelvic infection, skin and soft tissue infection. Piperacillin sodium has good stability in combination with sulbactam sodium and tazobactam sodium respectively, and shows strong antibacterial activity against common clinical enzyme-producing bacteria, expanding the antibacterial spectrum, and has wide applicatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/68A61K31/496A61P31/04
CPCC07D499/68
Inventor 陈立平
Owner 陈立平
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