Purification method of faropenem sodium hydrate

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...

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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

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