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Synthesizing method of vinorelbine tartrate

A technology of vinorelbine tartrate and a synthesis method, which is applied in the field of synthesis of vinblastine and vindoline to synthesize vinorelbine tartrate, can solve the problems of high price of synthetic raw materials, difficulty in obtaining, etc., and achieves cost reduction, cheap raw materials, and reduced production. cost effect

Inactive Publication Date: 2007-09-19
刘全胜
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0017] Based on this, the present invention finds better process conditions through screening and research, and solves the problem that the synthetic raw materials of vinorelbine tartrate are expensive and difficult to obtain

Method used

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  • Synthesizing method of vinorelbine tartrate
  • Synthesizing method of vinorelbine tartrate
  • Synthesizing method of vinorelbine tartrate

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Embodiment Construction

[0029] The present invention will be further described below in conjunction with specific embodiments.

[0030] (1) In a round bottom flask, add 34.8g of vinblastine tartrate (equivalent to 23.9g of vinblastine (M:336.43)) and 32.5g of vindoline, then add a small amount of dilute hydrochloric acid to dissolve, add 4.7L of trichloro Mix the iron oxide thoroughly and react for 13 hours under a sealed condition of 4°C. The reaction is terminated. A suitable amount of ammonia is added to the reaction solution to adjust the pH to 7, the reaction solution is centrifuged at high speed and the supernatant is discarded. The lower layer is soaked in chloroform several times. The chloroform phase is collected and evaporated to dryness to obtain the compound, which is the product of the first step reaction.

[0031] (2) Add 0.4 mol of hydrochloric acid to the product obtained after the chloroform phase is evaporated and dry, then add 5.7L of sodium borohydride to the dissolved material, react...

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Abstract

The invention discloses a synthesis method of vinorelbine bitartrate which is characterized in that the method includes following steps: (1) having the catharanthine tartrate and vindoline as initial material, reacting with ferric trichloride and hydrochloric acid; (2) reacting the above product with the sldium borohydride to get dehydrated vinblastine; (3) ring-opening the dehydrated vinblastine by trifluoroacetic anhydride and rearranging to obtain the vinorelbine bitartrate. The method has a low production cost and a high yield and has a good application future.

Description

Technical field [0001] The present invention relates to a method for synthesizing vinblastine tartrate obtained by deep processing of vinblastine and vindoline obtained from the anti-cancer plant drug source Catharanthus roseus. Background technique [0002] Vinorelbine tartrate is a cell cycle-specific broad-spectrum anti-tumor drug. It was developed by the French company Pieer Fabre and was first marketed in France in 1989. In 1993, my country began to approve its import. The synthesis methods of vinorelbine tartrate reported in the literature include the following four methods, which are summarized as follows: [0003] 1) Dehydrated vinblastine is oxidized by m-chloroperoxybenzoic acid (MCPBA) to obtain N-oxide, then treated with trifluoroacetic anhydride to open the ring, and then rearranged in the presence of water to obtain vinorelbine, which is then combined with tartaric acid Vinorelbine tartrate is obtained by salt formation. [0004] [0005] [0006] 2) Dehydrated ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/04
Inventor 刘全胜
Owner 刘全胜
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