Catalyst composition and method for preparing faropenem sodium

A faropenem sodium and catalyst technology, applied in the field of preparation of faropenem sodium, can solve the problems of excessive heavy metals, deterioration, unstable catalyst properties, etc., achieve high recovery rate, easy separation, and reduce pollution.

Active Publication Date: 2015-01-21
HUNAN WARRANT PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In this reaction, Pd(PPh 3 ) 4 Soluble in a system that uses a mixture of dichloromethane and acetic acid as a solvent, it is difficult to recover, which not only makes it difficult to recycle this expensive catalyst, but also has the risk of product being contaminated by the catalyst, causing the heavy metal in the product to exceed the standard
In addition, Pd(PPh 3 ) 4 The nature of the catalyst is unstable, and it will deteriorate if left for a long time

Method used

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  • Catalyst composition and method for preparing faropenem sodium
  • Catalyst composition and method for preparing faropenem sodium
  • Catalyst composition and method for preparing faropenem sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Add 10g of intermediate; 2.0g of triphenylphosphine and 2g of Pd-C (containing 10% palladium) to 60mL of dry methylene chloride in sequence, and add 60mL of ethyl acetate solution prepared by 0.5M sodium 2-ethylhexanoate , stirred at room temperature for 8 hours, stopped the reaction, filtered with suction, recovered Pd-C, added 2ml of water to the reaction solution, stirred until a solid precipitated, and continued to stir for 0.5 hours, filtered with suction to obtain a light yellow solid, which was dissolved in as much Add 0.5 g of activated carbon to a small amount of water, decolorize for 30 minutes, filter, add the filtrate to 5 times the amount of acetone, and place it for crystallization to obtain 7.0 g of faropenem sodium with a yield of 64.5%.

Embodiment 2

[0035] Add 10g of intermediate; 2.0g of triphenylphosphine and 2g of Pd-C (containing 10% palladium) to 60mL of dry dichloromethane successively, add 60mL of ethyl acetate solution prepared by 0.5M sodium p-benzenesulfinate, Stir at 40°C for 3 hours, stop the reaction, filter with suction, recover Pd-C, add 2ml of water to the reaction solution, stir until a solid precipitates, and continue stirring for 0.5 hours, filter with suction to obtain a light yellow solid, dissolve the solid in as much Add 0.5 g of activated carbon to a small amount of water, decolorize for 30 minutes, filter, add the filtrate to 5 times the amount of acetone, and place it for crystallization to obtain 6.5 g of faropenem sodium, with a yield of 60.2%.

Embodiment 3

[0037]Add 10g of the intermediate; 2.0g of triphenylphosphine and 4.2g of Pd-C (containing palladium 5%) to 60mL of dry methylene chloride in turn, and add 0.5M ethyl acetate solution prepared by sodium 2-ethylhexanoate 60mL, stirred at 25°C for 7 hours, stopped the reaction, filtered with suction, recovered Pd-C, added 2ml of water to the reaction solution, stirred until a solid precipitated, and continued to stir for 0.5 hours, filtered with suction to obtain a light yellow solid, which was dissolved in Add 0.5 g of activated carbon to as little water as possible, decolorize for 30 minutes, filter, add the filtrate to 5 times the amount of acetone, and place it for crystallization to obtain 7.0 g of faropenem sodium, with a yield of 64.5%.

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Abstract

The invention provides a catalyst composition, mainly containing palladium carbon (Pd / C) and triphenylphosphine, wherein the molar ratio of palladium to the triphenylphosphine is 1:2-1:6. The invention also provides a method for preparing faropenem sodium of a formula I, comprising the following step of: performing a reaction of a compound as an intermediate in a formula II and an allyl receptor under the action of a catalyst for removing allyl to produce the faropenem sodium of the formula I. The adopted catalyst for removing the allyl is the catalyst composition containing the palladium carbon (Pd / C) and the triphenylphosphine. The catalyst composition is easy to recover, thereby greatly reducing pollution of the palladium in a product.

Description

technical field [0001] The present invention relates to a catalyst composition, and a specific aspect of the present invention relates to a preparation method of faropenem sodium. Background technique [0002] Tetrakis(triphenylphosphine)palladium (Pd(PPh 3 ) 4 ) is a homogeneous catalyst with important uses in the field of organic synthesis, often used to catalyze various couplings, such as Suzuki coupling, Stille coupling, Kumada coupling, Negishi coupling, Murahashi coupling, Hiyama coupling and Sonogashira coupling et al. However, in the existing use of Pd(PPh 3 ) 4 Under certain reaction conditions, the catalyst is usually soluble in the reaction system and is not easily separated after the reaction is completed, so this expensive catalyst cannot be recycled, and sometimes it will cause heavy metal pollution to the product. This is the case, for example, for its use in the synthesis of faropenem sodium. [0003] Faropenem sodium is a new oral antibacterial drug. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D499/893C07D499/16B01J31/28A61P31/04
Inventor 黄本东
Owner HUNAN WARRANT PHARMA
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