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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  • 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-

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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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Example Embodiment

[0026] Example 1: A method for differential conversion of 7-differential taxane to form taxane, the specific steps are as follows:

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

[0028] (2) Dissolve cobalt chloride in step (1) Solution A to obtain a reaction system, and place the reaction system at a temperature of 0°C for 72 hours to obtain solution B; wherein the concentration of cobalt chloride in the reaction system is 20g / L;

[0029] (3) Concentrate and dry the solution B in step (2) under vacuum and carry out column chromatography elution and separation to obtain unconverted 7-epaclitaxel, paclitaxel and cobalt chloride, and return of the unconverted 7-epaclitaxel and cobalt chloride The conversion is continued in step (2); wherein the eluent is a dichloromethane-methanol solvent, the volume ratio of dichloromethane to methanol in the dichloromethane-methanol solvent is 9:1 (v / v); ...

Example Embodiment

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

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

[0034] (2) Dissolve cobalt chloride in step (1) Solution A to obtain a reaction system, and place the reaction system at a temperature of 20°C for 28 hours 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 in step (2) under vacuum and carry out column chromatography elution and separation to obtain unconverted 10-deacetyl-7-epi-paclitaxel, 10-deacetyl-paclitaxel and cobalt chloride, and unconverted 10 -Deacetyl-7-differential paclitaxel and cobalt chloride return to step (2) to continue the conversion; wherein the eluent is a dichloromethane-methanol solvent, ...

Example Embodiment

[0038] Embodiment 3: A method for the differential conversion of 7-differential baccatine III to baccatine III, the specific steps are as follows:

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

[0040] (2) Dissolve cobalt chloride into step (1) Solution A to obtain a reaction system, and place the reaction system at a temperature of 50°C for 100 hours to obtain solution B; wherein the concentration of cobalt chloride in the reaction system is 100g / L;

[0041] (3) Concentrate and dry the solution B in step (2) under vacuum and carry out column chromatography elution and separation to obtain unconverted 7-epibacatin III and cobalt chloride, and unconverted 7-epibacatin Catine III and cobalt chloride are returned to step (2) for static conversion; wherein the eluent is a dichloromethane-methanol solvent, and the volume ratio of dichloromethane to methanol in...

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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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