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Method for differential conversion of 7-epitaxol into taxane

A taxane and paclitaxel technology, applied in the field of medicine, can solve the problems of multiple product conversion yields, complicated processes, etc., and achieve the effects of good economic benefits, simple technology, and reduced production costs

Pending Publication Date: 2019-08-09
YUNNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the technical problems in the prior art that the epi-conversion of 7-epia taxanes to form taxanes is easy to form multiple products, the conversion yield is low, and the process is complicated, the present invention provides a simple and low-cost 7-epia The method of epi-conversion to taxane to form taxane, which converts 7-epimine taxane, which has no medicinal value, into an enantiomer with medicinal value, so as to save taxus resources and reduce the cost of paclitaxel. and docetaxel production cost purposes

Method used

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  • Method for differential conversion of 7-epitaxol into taxane
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  • Method for differential conversion of 7-epitaxol into taxane

Examples

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Embodiment 1

[0026] Embodiment 1: A kind of method of 7-epitaxane epitropic transformation forms taxane, and specific steps are as follows:

[0027] (1) Dissolving 7-epi-paclitaxel in methanol to obtain solution A; wherein the concentration of 7-epi-paclitaxel in solution A is 1 g / L;

[0028] (2) Cobalt chloride is dissolved in the step (1) solution A to obtain the reaction system, and the reaction system is allowed to stand and transform for 72h at a temperature of 0°C to obtain solution B; wherein the concentration of cobalt chloride in the reaction system is 20g / L;

[0029] (3) After step (2) solution B is concentrated and dried in vacuum, carry out column chromatography elution separation to obtain unconverted 7-epitaxol, paclitaxel and cobalt chloride, and unconverted 7-epitaxol and cobalt chloride return Continue conversion in step (2); Wherein eluent is dichloromethane-methanol solvent, and the volume ratio of dichloromethane and methanol in the dichloromethane-methanol solvent is...

Embodiment 2

[0032] Example 2: A method for the epi-conversion of 10-deacetyl-7-epi-paclitaxel to form 10-deacetyl-paclitaxel, the specific steps are as follows:

[0033] (1) Dissolving the mixture containing 10-deacetyl-7-epi-paclitaxel in ethanol to obtain solution A; wherein the concentration of 10-deacetyl-7-epi-paclitaxel in solution A is 10 g / L;

[0034] (2) Cobalt chloride is dissolved in the solution A of step (1) to obtain the reaction system, and the reaction system is allowed to stand and transform for 28h at a temperature of 20°C to obtain solution B; wherein the concentration of cobalt chloride in the reaction system is 1g / L;

[0035] (3) Concentrate and dry the solution B of step (2) in vacuo and then carry out column chromatography elution and separation to obtain unconverted 10-deacetyl-7-epitaxol, 10-deacetylpaclitaxel and cobalt chloride, unconverted 10 -deacetylation-7-poor to paclitaxel and cobalt chloride return step (2) to continue conversion; Wherein the eluent is ...

Embodiment 3

[0038] Embodiment 3: a kind of method of 7- epibaccatin III epitropy conversion forms baccatin III, and concrete steps are as follows:

[0039] (1) Dissolving 7-epibacatin III in dimethyl sulfoxide to obtain solution A; wherein the concentration of 7-epistobacatin III in solution A is 30 g / L;

[0040] (2) cobalt chloride is dissolved in the solution A of step (1) to obtain the reaction system, and the reaction system is left to stand and transformed for 100h under the condition of 50 ℃ to obtain solution B; wherein the concentration of cobalt chloride in the reaction system is 100g / L;

[0041] (3) After step (2) solution B is concentrated and dried in vacuum, carry out column chromatography elution separation to obtain unconverted 7-epiabacatin III baccatin III and cobalt chloride, and unconverted 7-epiabacatin III Cardine III and cobalt chloride return step (2) and leave standstill conversion; Wherein eluent is dichloromethane-methanol solvent, and the volume ratio of dichl...

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Abstract

The invention discloses a method for differential conversion of 7-epitaxol into taxane and belongs to the technical field of medicaments. The method comprises the steps of dissolving a reaction raw material containing 7-epitaxol in an organic solvent to obtain a solution A; dissolving cobalt chloride into the solution A to obtain a reaction system, and performing standing and conversion on the reaction system to obtain a solution B; concentrating and drying the solution B in vacuum, and then performing column chromatography elution and separation to obtain an unconverted 7-epitaxol compound, taxane and cobalt chloride, and returning the unconverted 7-epitaxol compound and the cobalt chloride for continuing conversion. According to the method, a chemical differential conversion approach isadopted for converting the 7-epitaxol without a medicinal value into an enantiomer with a medicinal value, so that the purposes of saving taxus resources and reducing the production costs of paclitaxel and docetaxel are achieved.

Description

technical field [0001] The invention relates to a method for epitaxy conversion of 7-epiataxane to form taxane, which belongs to the technical field of medicines. Background technique [0002] Paclitaxel is an expensive anti-cancer drug extracted from the yew plant. The raw materials for production are seriously insufficient, the production process is long, and the production cost is high, which leads to the high price of paclitaxel. By transforming the 7-epimized taxanes, which currently have no medicinal value and exist in a large amount in the branches and leaves of Taxus chinensis, into corresponding taxanes, the yield of paclitaxel can be increased, which has great economic value. There are many kinds of epitaxane compounds, among which 7-epitaxol, 10-deacetyl-7-epitaxol, 7-epiacephalomannine, 10-deacetyl-7- Different to cephalomannine, 10-deacetyl-7-different to baccatin III and so on. Their common feature in structure is that the 7-position hydroxyl group on the tax...

Claims

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Application Information

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IPC IPC(8): C07D305/14
CPCC07D305/14Y02P20/55
Inventor 王兴红
Owner YUNNAN UNIV
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