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Process for preparing cilastatin sodium

A technology of cilastatin and sodium heptenoate, applied in the directions of sulfide preparation, chemical instruments and methods, preparation of organic compounds, etc., can solve the problem of not industrialized production of cilastatin sodium, reducing product yield and purity, Failure to meet economic requirements, etc.

Active Publication Date: 2008-11-19
SHENZHEN HAIBIN PHARMA
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Problems solved by technology

[0014] But in the above-mentioned method of PCT / WO 2006 / 022511 A1, because in carrying out the alkali exchange operation process of cation exchange resin, the heat released by acid-base reaction can cause a small amount of cilastatin (VI) to decompose and reduce the yield of product and Purity; In addition, the process operation of preparing cilastatin sodium (I) by cilastatin ammonium (XIV) is loaded down with trivial details, does not reach the requirement of economy, so still not a better industrialized production of cilastatin sodium ( I) method

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  • Process for preparing cilastatin sodium
  • Process for preparing cilastatin sodium
  • Process for preparing cilastatin sodium

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Embodiment Construction

[0037] The present invention is further described by the following examples to make the present invention clearer and easier to understand.

[0038] Step 1 Preparation of (Z)-7-chloro-2((S)-2,2-dimethylcyclopropylcarboxamido)-2-heptenoic acid (IV)

[0039] (Z)-7-chloro-2((S)-2,2-dimethylcyclopropylcarboxamido)-2-heptenoic acid (IV) was used according to the method reported in EP 48301B1 with 247.8g 7-chloro- Ethyl 2-oxoheptanoate (III), 135.6g (+)-2,2-dimethylcyclopropanecarboxamide and 1.6g p-toluenesulfonic acid were synthesized in 1200mL toluene, concentrated and reclaimed toluene to give 359.3 g brown viscous liquid, the product was directly used in the next reaction without separation.

[0040] Add 359.3g of the brown viscous liquid obtained in the previous step into 600mL of ethanol and 720g of 10% sodium hydroxide solution, heat to 45-50°C, heat and stir to make it react, monitor the reaction process by HPLC, and the reaction is completed in about 10 hours; then Add t...

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Abstract

The invention relates to a method for preparing a compound called cilastatin sodium shown as a formula (I). Cilastatin is prepared by crystallizing and purifying (Z)-7-chlorine-2((S)-2, 2-dimethyl c-pr carbamoyl)-2-heptenoic acid and the cilastatin sodium is prepared by purifying the cilastatin through microporous resin, thereby improving the purity quotient and the yield coefficient of the cilastatin sodium.

Description

technical field [0001] The invention relates to a method for preparing a compound, in particular to a method for preparing cilastatin sodium (Cilastain Sodium Salt). Background technique [0002] The chemical name of cilastatin sodium is [R-[R * , S * (Z)]]-7[(2-amino-2-carboxyethyl)sulfur]-2-[[(2,2-dimethylcyclopropyl)carbonyl]amino]-2-heptenoate sodium, Its chemical structure is as formula (I), molecular formula is C 12 h 25 N 2 NaO 5 S, the molecular weight is 380.44. The combination of cilastatin sodium and β-carbapenem antibiotics such as imipenem can inhibit the degradation of imipenem by renal dehydrodipeptidase and increase the concentration of imipenem in the urinary tract , thereby increasing the activity of imipenem and reducing its nephrotoxicity. Imipenem / cilastatin sodium has been widely used as a broad-spectrum antibacterial agent. [0003] [0004] Existing a lot of reports about the preparation method of cilastatin sodium at present. EP 48301 B1...

Claims

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Application Information

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IPC IPC(8): C07C323/59C07C319/20
CPCC07C319/28C07C319/14C07C319/20
Inventor 卢兆强张恒利
Owner SHENZHEN HAIBIN PHARMA
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