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Purification method of faropenem sodium hydrate

A technology of faropenem sodium and ropenem sodium, which is applied in the field of drug hydrates, can solve problems such as easy decomposition, difficult recovery, and difficult recrystallization, and achieve the effect of increasing crystallization yield and reducing costs

Inactive Publication Date: 2014-02-19
HUANGGANG LUBAN PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Faropenem sodium hydrate is unstable in solution or at high temperature, easy to decompose, and difficult to recrystallize. The existing crystallization method mainly uses water and acetone (reference: EP0410727), but because the product crystallizes in water, it needs to add 2.5 It can be dissolved when the temperature is raised to 50-60°C. Because the product is unstable in water at high temperature, some products will be degraded, and the yield is low, about 70-75%. There are more products in the mother liquor, because it contains more degradation at the same time Impurities, difficult to recover

Method used

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  • Purification method of faropenem sodium hydrate
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  • Purification method of faropenem sodium hydrate

Examples

Experimental program
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Effect test

Embodiment 1~11

[0017] Step 1) In a dry 500mL three-neck flask, add the crude faropenem sodium hydrate (content 98.0%) and lower alcohol solvent, T 1 After stirring and dissolving at °C, 2.5 g of activated carbon was added, stirred at room temperature for 15 minutes, and filtered to obtain the filtrate.

[0018] Step 2) Add deionized water to the filtrate and control the temperature at T 2 The lower alcohol solvent was evaporated under reduced pressure at ℃ to obtain a residue.

[0019] Step 3) Add a poorly soluble ketone solvent to the residue and cool to T 3 ℃ and controlled to crystallize at this temperature, keep for t hours, filter, vacuum dry to obtain off-white crystals.

[0020] Table 1 Crystallization process parameters of Examples 1-11

[0021]

[0022] figure 1 Is the mass spectrum of the pure product of Faropenem Sodium Hydrate obtained in Example 1; figure 2 This is the NMR spectrum of the pure faropenem sodium hydrate obtained in Example 1.

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Abstract

The invention discloses a purification method of a faropenem sodium hydrate, which comprises the following steps: 1) dissolving a faropenem sodium hydrate crude product in a lower alcohol solvent at -20-40 DEG C, adding active carbon for decoloration, filtering, 2) adding water into filtrate, performing decompression concentration and evaporation at 0-40 DEG C to remove the lower alcohol solvent, and 3) adding residual into a ketone insoluble solvent, stirring, crystallizing and filtering to form the pure faropenem sodium hydrate, wherein for the faropenem sodium hydrate crude product, the water content is 1g:(0.5-2mL). According to the method, the faropenem sodium hydrate crude product is dissolved in the lower alcohol solvent at the low temperature, a little water is added, and the lower alcohol solvent is evaporated off at the low temperature; the whole purification process is performed at the low temperature all the time, so that the crystallization yield is increased obviously and reaches above 90%; and residual products in a mother solution are fewer, so that the product cost is lowered.

Description

Technical field [0001] The invention belongs to the technical field of drug hydrates, and specifically relates to a purification method of faropenem sodium hydrate. Background technique [0002] Faropenem sodium hydrate (Faropenem sodium hydrate) is a penicillene antibiotic developed by Suntory of Japan, which was launched in Japan on September 15, 1997. Its structural formula is: [0003] [0004] Full chemical name: (5R, 6S)-6-[(1R)-1-hydroxyethyl]-7-oxo-3-[(2R)-2-tetrahydrofuranyl]-4-thia-1-aza Bicyclo[3.2.0]hept-2-ene-2-carboxylic acid monosodium salt two sesquihydrate is the first oral penicillene antibiotic to be marketed in China. It is located on the 2-position of the penicillene core Connected with a 4-hydrofuran group, the chemical structure is relatively stable, and the basic structure is similar to β-lactam antibiotics. It belongs to atypical β-lactam antibiotics. It has good affinity for penicillin and has good β-lactam Amidase stability is a national four-class new...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/893C07D499/18
CPCC07D499/18C07D499/893
Inventor 杨小龙李强刘向群胡新良陈潜
Owner HUANGGANG LUBAN PHARM
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