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Preparation method of vinorelbine tartrate

A technology of vinorelbine tartrate and vinorelbine, which is applied in the field of preparation of vinorelbine tartrate, can solve the problems of low purity of vinorelbine, difficulty in industrial production, and great difficulty in purification, and achieve simplified operation, simple operation, and reduced production cost effect

Pending Publication Date: 2021-03-26
海南长春花药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Integrating the existing preparation methods, basically there are many by-products in the reaction process, which are difficult to control, resulting in low purity of vinorelbine and great difficulty in purification, thus making the cost high and difficult to industrialized production

Method used

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  • Preparation method of vinorelbine tartrate
  • Preparation method of vinorelbine tartrate
  • Preparation method of vinorelbine tartrate

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preparation example Construction

[0045] A preparation method of vinorelbine tartrate, comprising:

[0046] 1) Preparation steps of dehydrated vinblastine: using vinblastine sulfate and pendolin as starting materials, catalyzed by ferric chloride and reduced by sodium borohydride, to prepare dehydrated vinblastine;

[0047] 2) The preparation steps of bromoanhydrovinblastine: dehydrovinblastine and N-bromosuccinimide (NBS) carry out bromination reaction to obtain the bromoanhydrovinblastine crude product; the bromoanhydrovinblastine crude product is purified through a column to improve Its purity, obtains bromoanhydrovinblastine;

[0048] 3) The preparation steps of vinorelbine: debromination and rearrangement of bromoanhydrovinblastine and silver tetrafluoroborate aqueous solution to obtain crude product of vinorelbine; recrystallization of crude product of vinorelbine to obtain pure product of vinorelbine;

[0049] 4) Preparation steps of vinorelbine tartrate: the pure product of vinorelbine is reacted with...

Embodiment 1

[0079] A preparation method of vinorelbine tartrate, comprising:

[0080] 1) The preparation steps of dehydrovinblastine: the specific preparation process is as follows:

[0081] 1-1) Preparation steps of liquid A: Take 4.4g of ventolin and 4g of vinblastine sulfate, add 40ml of tetrahydrofuran, add 20ml of hydrochloric acid solution, heat slightly, and dissolve under the condition of 35°C-40°C.

[0082] 1-2) Preparation steps of liquid B: Take 17g of ferric chloride, add 400ml of slightly heated purified water, add 10ml of hydrochloric acid solution, and use nitrogen to drive oxygen for about 10 minutes.

[0083] 1-3) Preparation steps of liquid C: Take 25g of ammonium chloride, add 80ml of slightly heated purified water to dissolve, add nitrogen to drive oxygen for about 10 minutes.

[0084] 1-4) Preparation steps of liquid D: Weigh about 1.2g of sodium borohydride and dissolve it in 70ml of dilute ammonia water. Dilute ammonia water refers to the mixed aqueous solution of...

Embodiment 2

[0105] A preparation method of vinorelbine tartrate, comprising:

[0106] 1) The preparation steps of dehydrovinblastine: the specific preparation process is as follows:

[0107] 1-1) Preparation steps of liquid A: Take 4.4g of ventolin and 4g of vinblastine sulfate, add 40ml of trifluoroethanol, and add 20ml of hydrochloric acid solution to slightly heat (35°C-40°C) to dissolve.

[0108] 1-2) Preparation steps of liquid B: Take 17g of ferric chloride, add 400ml of slightly heated purified water, add 10ml of hydrochloric acid solution, and use nitrogen to drive oxygen for about 10 minutes.

[0109] 1-3) Preparation steps of liquid C: Take 25g of ammonium chloride, add 80ml of slightly heated purified water to dissolve, add nitrogen to drive oxygen for about 10 minutes.

[0110] 1-4) Preparation steps of liquid D: Weigh about 1.3g of sodium borohydride and dissolve it with 70ml of dilute ammonia water. Dilute ammonia water refers to the mixed aqueous solution of ammonia water w...

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Abstract

The invention discloses a preparation method of vinorelbine tartrate, which comprises the following steps: 1) preparation of dehydrated vinblastine: taking vinblastine sulfate and vindoline as initialraw materials, and carrying out ferric trichloride catalysis and sodium borohydride reduction to obtain dehydrated vinblastine; 2) preparation of bromo-dehydrated vinblastine: carrying out bromination reaction on dehydrated vinblastine and N-bromo-succinimide to obtain a bromo-dehydrated vinblastine crude product; carrying out column purification on the bromo-dehydrated vinblastine crude productto improve the purity of the bromo-dehydrated vinblastine crude product so as to obtain bromo-dehydrated vinblastine; 3) preparation of vinorelbine: carrying out debromination rearrangement on bromo-dehydrated vinblastine and a silver tetrafluoroborate aqueous solution to obtain a vinorelbine crude product; and recrystallizing the vinorelbine crude product to obtain a vinorelbine pure product; and4) preparation of vinorelbine tartrate: carrying out a salt forming reaction on the pure vinorelbine tartrate and tartaric acid to obtain vinorelbine tartrate. The method has the advantages of simpleoperation, few side reactions, great increase of the purity and the yield, reduction of the production cost, and suitableness for large-scale production.

Description

technical field [0001] The invention relates to the technical field of chemical synthesis, in particular to a preparation method of vinorelbine tartrate. Background technique [0002] Vinorelbine tartrate is a cell cycle-specific broad-spectrum antineoplastic drug that was first launched in France in 1989. Its main function is to bind to tubulin, thereby making the formation of microtubules in the process of cell mitosis difficult. Vinorelbine is a vinblastine derivative with a similar effect to vincristine. Vinorelbine is a cycle-specific drug, commonly used clinically for the treatment of non-small cell lung cancer (NSCLC) and breast cancer, ovarian cancer, head and neck cancer, leukemia, and for small cell lung cancer, colon cancer, brain tumor, and malignant melanoma. etc. also have a strong inhibitory effect. [0003] Current literature reports that vinorelbine tartrate is basically prepared from anhydrovinblastine (3',4'-anhydrovinblastine), that is, using it as an ...

Claims

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Application Information

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IPC IPC(8): C07D519/04
CPCC07D519/04
Inventor 邓团飞郑钞何演安
Owner 海南长春花药业有限公司
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