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Method for preparing vindoline and Catharanthine

A technology of vinblastine and vindolin, which is applied in the field of natural medicines, can solve the problems such as insufficient comprehensive utilization of resources, and achieve the effect of low process cost.

Inactive Publication Date: 2008-03-26
上海安体康生植物化学有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Domestic production of vinca total alkaloids only extracts vinblastine with a low content from vinca plants, while a large amount of monoindole alkaloids, vindolin and vinblastine, are discarded as waste, resulting in poor comprehensive utilization of resources

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Take 10kg of whole periwinkle herb, crush it, and extract it by cold soaking with 201 mass percent of 0.7% sulfuric acid for 3 times, combine the extracts, adjust the pH to 7-8 with ammonia water, then use 101 chloroform for countercurrent continuous extraction, concentrate under reduced pressure, and then With a small amount of acetone pumped loose, total weak alkaloids 20.5g. Dissolve the total weak alkaloids in 10ml of absolute ethanol to form a concentrated solution, then add 5% sulfuric acid ethanol solution to pH 3.8-4.1 and let it stand overnight to precipitate crystals, and filter to obtain 1.5g of mixed vinblastine sulfate.

[0013] The filtrate was adjusted to pH 7-8 with aqueous ammonia, extracted with chloroform, and concentrated under reduced pressure to obtain 15 g of free alkaloid. Dry mix the sample in 50g macroporous adsorption resin (DA201), elute with volume ratio ethanol: water (15:85, 30:70, 50:50, 70:30, 95:5), collect in 360ml volume, depressurize...

Embodiment 2

[0015] Take 10kg of whole periwinkle herb, crush it, and extract it by cold soaking with 201 mass percent of 0.7% sulfuric acid for 3 times, combine the extracts, adjust the pH to 7-8 with ammonia water, then use 101 chloroform for countercurrent continuous extraction, concentrate under reduced pressure, and then With a small amount of acetone pumped loose, total weak alkaloids 20.5g. Dissolve the total weak alkaloids in 10ml of absolute ethanol to form a concentrated solution, then add 5% sulfuric acid ethanol solution to pH 3.8-4.1 and let it stand overnight to precipitate crystals, and filter to obtain 1.5g of mixed vinblastine sulfate.

[0016] The filtrate was adjusted to pH 7-8 with aqueous ammonia, extracted with chloroform, and concentrated under reduced pressure to obtain 15 g of free alkaloid. Dry mixed sample in 50g macroporous adsorption resin (HZ-841), eluted with volume ratio ethanol: water (15:85, 30:70, 50:50, 70:30, 95:5), collected in 50ml volume, Concentrat...

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PUM

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Abstract

A process for preparing vindoline and vinblastine, which can be used to prepare the antineoplastic medicines, from Chinese ivy flower includes such steps as immersing in sulfuric acid solution, regulating pH=7-8, extracting in chloroform, vacuum concentrating, dissolving in absolute alcohol, adding the solution of sulfuric acid in alcohol antil pH=3.8-4.1, laying aside for educing out crystals, filtering to obtain vinblastine sulfate, regulating pH of fitlrate to 7-8, extracting in chlorofmr, vacuum concentrating, absorbing by macroreticular resin, eluting with mixture of polar solvent and water, and vacuum concentrating.

Description

1. Technical field: [0001] The invention relates to a preparation method of Wenduoling and vinblastine, belonging to the technical field of natural medicines. It specifically relates to a new process for extracting vinblastine and wenduoling from periwinkle flowers. Vinblastine and wenduoling are important raw materials for synthesizing antitumor drugs vinorelbine, vinblastine and vincristine. 2. Background technology: [0002] Vinblastine antineoplastic drugs are bisindole alkaloids with anticancer activity and their structurally modified derivatives isolated from Catharanthus roseus or Vinca rosea L.. The natural ones are Vinblastine (VLB) and Vincristine (VCR). Vinblastine is used to treat various solid tumors, and vincristine is mainly used to treat acute leukemia in children. Vinblastine is a bimolecular indole alkaloid composed of Vindoline and velbenamine. In the 1970s, Eli Lilly researched and developed the Vindesine drug (vinblastine, Vindestine, VDS) for the tre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/20C07D209/00
Inventor 倪新忠胡立宏
Owner 上海安体康生植物化学有限公司