Process for preparing sodium azlocillin

Abstract

The preparation process of sodium azlocillin includes the following steps: 1. adding triethylamine slowly into water solution of ampicillin at 0-4 deg.c and stirring to clarify the reaction liquid; 2. adding 2-imidazolidinyl ketacyl chloride into the solution at 0-4 deg.c while dropping water solution of Na2CO3 or NaHCO3 to control pH 7.5-8.5 and performing condensation; 3. adding ethyl acetate into the reaction mixture at 0-5 deg.c and regulating pH value to 1.7-1.9; 4. separating to obtain organic phase, and eliminating heat source and impurity to obtain crystallization liquid; and 5. adding ethyl acetate solution of sodium isocaprylate to crystallize, separating and drying to obtain powdered white sodium azlocillin. The process has convenient operation, mild reaction condition, high yield and high product quality.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and more specifically, the invention provides a preparation method of azlocillin sodium. Background technique [0002] The chemical name of azlocillin sodium (benmidazole penicillin) is (2S, 5R, 6R)-3,3-dimethyl-6-[(R)-2-(2-oxo-1-imidazolidine carboxamide Base-2-phenylacetamido)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid sodium salt, its chemical formula is shown in formula (I). Azlocillin sodium is not destroyed by penicillinase produced by Staphylococcus aureus, and is effective against enzyme-producing Staphylococcus aureus, mainly used for surrounding infections of penicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis, including internal organs, skin and soft tissues Infections in other parts, such as amikacin, gentamicin, and netilmicin, can produce synergistic effects. [0003] [0004] Molecular formula: C 20 h 22 N 5 NaO 6 S molecular weight:...

AI Technical Summary

Problems solved by technology

[0017] The method of route 2 has long steps and high operating conditions, so it is not suitable for use

[0018] The method yield of route 3 is low (42%), and activator preparation is difficult, and operation requirement is higher, should not adopt

[0019] Although the method yield of route 4 is high, the reaction conditions are harsh, and the source of reagent dimethylaminopropanol is difficult, so it should not be used

[0020] The method of route 6 is simple in operation and high in yield, but the preparation of raw material ethyl diisocyanate is complicated and should not be used

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