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Ledipasvir key intermediate and preparation method thereof

An intermediate and key technology, applied in the field of preparation of Ledipavir intermediates, can solve problems such as imperfect process technology, and achieve the effects of safe and reliable production process, mature and stable process, and stable product quality

Inactive Publication Date: 2018-04-06
安徽诺全药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The intermediate of Reddy Pavi is a variety whose patent protection has expired, and the domestic process technology is not yet perfect

Method used

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  • Ledipasvir key intermediate and preparation method thereof
  • Ledipasvir key intermediate and preparation method thereof
  • Ledipasvir key intermediate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A preparation method of the key intermediate LD-J of Radipa Wei, comprising the steps of:

[0028] (1) Preparation of LD-G

[0029] Synthesis process:

[0030]

[0031] Preparation steps: Add LD-SM2 and N-methylpyrrolidone into the reaction kettle, stir until dissolved, add the brominating reagent N-bromosuccinimide in batches, then add the catalyst benzoyl peroxide, and control the reaction temperature Stir the reaction at 60°C for 7 hours, monitor the completion of the reaction by HPLC, cool down to 18°C, add water, separate layers, add methanol to the lower layer liquid, a large amount of solids precipitate out, centrifuge and dry to obtain a white solid LD-G;

[0032] (2) Preparation of LD-H

[0033] Synthesis process:

[0034]

[0035] Preparation steps: Add LD-G and acetic acid into the reaction kettle, heat to 40°C, and stir for 25 minutes to dissolve, adjust the temperature of the reaction kettle to 20°C, add 18% sulfuric acid, then add iodine, potassiu...

Embodiment 2

[0049] A preparation method of Reddy Pavell, comprising the steps of:

[0050] (1) Preparation of LD-G

[0051] Synthesis process:

[0052]

[0053] Preparation steps: Add LD-SM2 and N-methylpyrrolidone into the reaction kettle, stir until dissolved, add the brominating reagent N-bromosuccinimide in batches, then add the catalyst benzoyl peroxide, and control the reaction temperature Stir the reaction at 60-70°C for 7-9 hours, monitor the completion of the reaction by HPLC, cool down to 18-22°C, add water, separate layers, add methanol to the lower layer liquid, a large amount of solids precipitate, centrifuge and dry to obtain a white solid LD-G;

[0054] (2) Preparation of LD-H

[0055] Synthesis process:

[0056]

[0057] Preparation steps: Add LD-G and acetic acid into the reaction kettle, heat to 42°C, and stir for 30 minutes, dissolve, adjust the temperature of the reaction kettle to 25°C, add 20% sulfuric acid, then add iodine, potassium iodate, and The reacti...

Embodiment 3

[0071] (1) Preparation of LD-G

[0072] Synthesis process:

[0073]

[0074] Preparation steps: Add LD-SM2 and N-methylpyrrolidone into the reaction kettle, stir until dissolved, add the brominating reagent N-bromosuccinimide in batches, then add the catalyst benzoyl peroxide, and control the reaction temperature Stir the reaction at 70°C for 9 hours, monitor the completion of the reaction by HPLC, cool down to 22°C, add water, separate layers, add methanol to the lower layer liquid, a large amount of solids precipitate, centrifuge and dry to obtain a white solid LD-G;

[0075] (2) Preparation of LD-H

[0076] Synthesis process:

[0077]

[0078] Preparation steps: Add LD-G and acetic acid into the reactor, heat to 40-45°C, and stir for 25-35 minutes to dissolve, adjust the temperature of the reactor to 20-30°C, add 18-22% sulfuric acid, then Add iodine and potassium iodate, heat the reaction solution at 56-60°C for 3.5-4.5h, monitor the completion of the reaction by ...

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Abstract

The invention discloses a ledipasvir key intermediate LD-J, a structure of the ledipasvir key intermediate LD-J and a preparation method of the ledipasvir key intermediate LD-J. The preparation methodcomprises the following steps: (A1) preparing LD-G; (A2) preparing LD-H; (A3) preparing LD-I; (A4) preparing a Grignard reagent; and (A5) preparing LD-J. The ledipasvir key intermediate LD-J and thepreparation method thereof have the advantages that the process is mature and stable, the product is stable in quality, the production process is safe and reliable, and the preparation method is suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of preparation of raw materials and intermediates, in particular to a preparation method of a Radipavi intermediate. Background technique [0002] Redipavir (also known as sofosbuvir) is mainly used to treat hepatitis C infection. Hepatitis C virus hepatitis C or hepatitis C for short, is a kind of viral hepatitis caused by hepatitis C virus (HCV) infection. According to the statistics of the World Health Organization, the global HCV infection rate is about 3%, with a total of about 180 million people. Approximately 3.2 million people in the United States have hepatitis C. HCV infection mainly includes immune-mediated and HCV direct injury. After infection, the liver becomes inflamed, leading to decreased liver function or even failure. The pathological manifestations are mainly hepatocyte necrosis and lymphocyte infiltration. Most people with hepatitis C do not notice symptoms of liver damage until long ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C45/45C07C49/813
CPCC07C49/813C07C17/10C07C17/12C07C45/45C07C25/22
Inventor 杜小鹏许良志胡志刚何大荣钱祝进何勇刘庄子
Owner 安徽诺全药业有限公司
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