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Preparation method of vinblastine derivative

A technology of vinblastine and its derivatives, which is applied in the field of preparation of nordehydrovinblastine, can solve problems such as low yield, and achieve the effects of simplifying reaction steps, facilitating industrial production, and easy operation

Active Publication Date: 2017-05-31
河南绿园药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Among them, method 2 is reported to have a lower yield, and more literature focuses on method 1 with a higher yield

Method used

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  • Preparation method of vinblastine derivative
  • Preparation method of vinblastine derivative
  • Preparation method of vinblastine derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Under the condition of avoiding light, add 10mmol of the compound of formula A and 11mmol of Wenduolin into 150ml of trifluoroethanol, control the temperature to 0°C, add dropwise 30ml of 0.5mol / L salt solution of ferric sulfate, and add 5mmol of supernatant Oxyformic acid, continue to stir and react at 0°C for 4 hours, add sodium hydroxide to adjust the pH to about 7, discard the supernatant after high-speed centrifugation; discard the residue obtained after discarding the supernatant, soak in 150ml trifluoroethanol, and control the temperature to 75°C, continue to add 150ml of 2mol / L sodium acetate solution, then add 30mmol of thiourea dioxide, react at 75°C for 2h, extract with dichloromethane 100mL×3, wash with saturated saline, dry and evaporate the solvent under reduced pressure; continue to add acetone 150ml, 15mmol of L-tartaric acid were reacted to form a salt, and anhydrous ether was added dropwise under stirring until the precipitate was fully separated, filte...

Embodiment 2

[0033] Under the condition of avoiding light, add 10mmol of the compound of formula A and 11mmol of Wenduolin to 150ml of trifluoroethanol, control the temperature to 0°C, add 30ml of 0.5mol / L iron sulfate salt solution dropwise under stirring, and add 2.5mmol of For peroxyformic acid, continue to stir and react at 0°C for 4 hours, add sodium hydroxide to adjust the pH to about 7, discard the supernatant after high-speed centrifugation; discard the residue obtained after discarding the supernatant, soak in 150ml trifluoroethanol, and control the temperature To 75°C, continue to add 150ml of 2mol / L sodium acetate solution, then add 30mmol of thiourea dioxide, react at 75°C for 2h, extract with 100mL×3 dichloromethane, wash with saturated brine, dry and evaporate the solvent under reduced pressure; continue to add 150ml of acetone and 15mmol of L-tartaric acid were reacted to form a salt, and anhydrous ether was added dropwise with stirring until the precipitate was fully separat...

Embodiment 3

[0035] Under the condition of avoiding light, add 10mmol of the compound of formula A and 11mmol of Wenduolin to 150ml of trifluoroethanol, control the temperature to 0°C, add dropwise 30ml of 0.5mol / L salt solution of ferric sulfate, and add 2.5mmol of For peroxyformic acid, continue to stir and react at 0°C for 4 hours, add sodium hydroxide to adjust the pH to about 7, discard the supernatant after high-speed centrifugation; discard the residue obtained after discarding the supernatant, soak in 150ml trifluoroethanol, and control the temperature To 75°C, continue to add 150ml of 2mol / L sodium acetate solution, then add 40mmol of thiourea dioxide, react at 75°C for 2h, extract with 100mL×3 dichloromethane, wash with saturated saline, dry and evaporate the solvent under reduced pressure; continue to add 150ml of acetone and 15mmol of L-tartaric acid were reacted to form a salt, and anhydrous ether was added dropwise with stirring until the precipitate was fully separated, filte...

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Abstract

The invention relates to a preparation method of a vinblastine derivative. The preparation method comprises the following steps of under the effect of ferric sulfate and peroxide formic acid, a compound shown as the formula A is coupled with vindoline; then, a reducing agent is added for performing reduction reaction to obtain the navelbine through preparation. The preparation method has the advantages that the yield is high; the purity of the obtained product is very high.

Description

technical field [0001] The invention relates to the preparation of a vinblastine derivative, in particular to a preparation method of nordehydrovinblastine. Background technique [0002] Periwinkle is an important medicinal plant of the genus Oleander periwinkle. It is native to South Asia, the east coast of Africa and tropical America. It is a light-loving plant that likes warmth and chills, and is suitable for growing in a slightly dry and sunny environment. . The extraction of biologically active alkaloids from periwinkle has been going on for nearly a century, and the research on the extracted alkaloids as anticancer drugs has a history of many years. [0003] Vinblastine has good anti-tumor activity, but its toxic and side effects are large, and its derivative nordehydrovinblastine is developed and listed (drug name Vinorelbine Tartrate). [0004] After retrieval, the preparation method of nordehydrovinblastine is basically to obtain dehydrovinblastine first, and then...

Claims

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Application Information

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IPC IPC(8): C07D519/04
CPCC07D519/04
Inventor 丰贵鹏贾若凌杨玉萍章艳玲苏天鹅马国扬
Owner 河南绿园药业有限公司
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