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Method for preparing Zaltoprofen

A technology of intermediate and ethyl acetate phase, applied in the field of preparation of zaltoprofen, can solve the problems of difficult removal of impurities, slow reaction, low yield and the like, and achieves rapid and thorough reaction, few impurities and high yield Effect

Active Publication Date: 2014-10-15
ZHEJIANG YATAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The present invention aims at the disadvantages of the existing Zaltobuprofen preparation method, such as low yield, slow reaction in large-scale production, and difficult removal of impurities, etc., and provides Zaltobuprofen with high yield, easy refining, and suitable for industrialized large-scale production. Preparation method of ibuprofen

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  • Method for preparing Zaltoprofen
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Examples

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Effect test

Embodiment 1

[0027] A method for preparing Zaltoprofen, comprising the steps of:

[0028] Step a, take 5-(1-propionyl)-2-phenylthiophenylacetic acid as starting raw material, carry out rearrangement reaction with iodine, triethyl orthoformate under the situation that cuprous oxide is made a catalyst, will be with 5 -(1-propionyl)-2-phenylthiophenylacetic acid 1125g, iodine 1947g, triethyl orthoformate 4200ml, cuprous oxide 108g, add into the three-necked flask, first use light to heat to 55°C, continue to light, stir Reaction for 2 hours, wherein, 100W infrared lamp is used to penetrate into the reaction liquid for heating by light, and the light intensity is 2000lx;

[0029] Step b, the reaction kettle is cooled to room temperature, adding an aqueous solution of sodium thiosulfate with a mass fraction of 40%, continuing to stir for 5h, extracting with ethyl acetate, combining the ethyl acetate phases, and washing with an aqueous solution of sodium chloride with a mass fraction of 26.5% E...

Embodiment 2

[0034] A method for preparing Zaltoprofen, comprising the steps of:

[0035] Step a, take 5-(1-propionyl)-2-phenylthiophenylacetic acid as starting raw material, carry out rearrangement reaction with iodine, triethyl orthoformate under the situation that cuprous oxide is made a catalyst, will be with 5 -(1-propionyl)-2-phenylthiophenylacetic acid 1125g, iodine 1947g, triethyl orthoformate 4200ml, cuprous oxide 108g, add into the there-necked flask, first use light to heat to 55°C, continue to light, stir Reaction for 5 hours, wherein, 100W infrared lamp was used to immerse into the reaction solution to heat for light heating, and the light intensity was 4000lx;

[0036] Step b, the reaction kettle is cooled to room temperature, adding an aqueous solution of sodium thiosulfate with a mass fraction of 40%, continuing to stir for 2h, extracting with ethyl acetate, combining the ethyl acetate phases, and washing with an aqueous solution of sodium chloride with a mass fraction of 5...

Embodiment 3

[0041] A method for preparing Zaltoprofen, comprising the steps of:

[0042] Step a, take 5-(1-propionyl)-2-phenylthiophenylacetic acid as starting raw material, carry out rearrangement reaction with iodine, triethyl orthoformate under the situation that cuprous oxide is made a catalyst, will be with 5 -(1-propionyl)-2-phenylthiophenylacetic acid 1125g, iodine 1947g, triethyl orthoformate 4200ml, cuprous oxide 108g, add into the three-necked flask, first use light to heat to 55°C, continue to light, stir Reaction for 4 hours, wherein, 100W infrared lamp is used to penetrate into the reaction liquid for heating by light, and the light intensity is 3000lx;

[0043] Step b, the reaction kettle is cooled to room temperature, adding an aqueous solution of sodium thiosulfate with a mass fraction of 40%, continuing to stir for 4h, extracting with ethyl acetate, combining the ethyl acetate phases, and washing with an aqueous solution of sodium chloride with a mass fraction of 15% Eth...

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Abstract

The invention relates to a preparation method for Zaltoprofen, and discloses a method for preparing Zaltoprofen. The method comprises the following steps: using 5-(1-propionyl)-2-thiophenyl phenylacetic acid as an initiator; preparing the Zaltoprofen through rearrangement, hydrolysis and cyclization. The rearrangement of the 5-(1-propionyl)-2-thiophenyl phenylacetic acid adopts illumination to heat; the illumination function is embedded into atom, has an effect on electron, and reduces activation energy required by reaction; reaction efficiency is high; meanwhile, the illumination function enables iodine to sublimate into gas state; the iodine in gas state can be in contact with substrate fully; the reaction is more complete and quick; influence on the rearrangement reaction of methyl iodide is reduced; yield coefficient is higher; the method is simple to operate, environmentally friendly, and suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation method of zaltoprofen, in particular to a method for preparing zaltoprofen. Background technique [0002] Zaltoprofen (10,11-dihydro-α-methyl-10-oxydibenzo[b,f]thiapine-2-acetic acid), molecular formula C 17 h 14 o 3 S, molecular weight is 298.36, its structural formula is: [0003] [0004] Zaltoprofen is a new generation of COX non-specific inhibitor developed by Chemiphar and Zeria in Japan. It is a potent non-steroidal analgesic anti-inflammatory drug. Compared with compounds related to pharmacological effects such as ibuprofen, indomethacin, loxoprofen sodium, diclofenac sodium, etc., the analgesic effect of zaltoprofen, especially on the pain response induced by bradykinin Stronger, and at the same time have a stronger effect on acute, subacute and chronic inflammation. Zaltoprofen also has a high safety index, extremely low damage to the gastrointestinal tract, and the probability of major adverse r...

Claims

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Application Information

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IPC IPC(8): C07D337/14
CPCC07D337/14
Inventor 吕旭幸王丽云叶江陈洁冯超敏戴兴祥
Owner ZHEJIANG YATAI PHARMA
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