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Preparation method of valienamine from acarbose and/or acarbose derivatives using trifluoroacetic acid

A technology of acarbose and trifluoroacetic acid, which is applied in the field of production of villetamide, can solve the problems of non-commercialization and production difficulties

Inactive Publication Date: 2006-11-01
B T GIN · CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many difficulties, such as the determination of activity and the expression of gene probes
Therefore, the current production is quite difficult
[0009] As mentioned above, methods for the in vitro production of villitamide by purified enzymes or chemicals have not been commercialized, and to date have been mainly synthesized by hydrolyzing validoxylamine and validamycin with strains Pseudomonas denitrophila and Flavobacterium saccharophilum and the production of villetamide

Method used

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  • Preparation method of valienamine from acarbose and/or acarbose derivatives using trifluoroacetic acid
  • Preparation method of valienamine from acarbose and/or acarbose derivatives using trifluoroacetic acid
  • Preparation method of valienamine from acarbose and/or acarbose derivatives using trifluoroacetic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: the method that uses TFA to produce visleytamide

[0030] Put 10 g of pure acarbose into 10% TFA solution to make the final concentration 5%. At a reaction temperature of 100° C., the system was allowed to react for 12 hours or more, followed by removal of TFA and water. Purification was then carried out by using an ion exchange resin to obtain 2.02 g of villetamide.

Embodiment 2

[0031] Embodiment 2: the method that uses TFA to produce visleytamide

[0032] 1 g of pure acarbose derivatives (monosaccharides and trisaccharides) was put into 10% TFA solution to make the final concentration 5%. At a reaction temperature of 100° C., the system was allowed to react for 12 hours or more, followed by removal of TFA and water. Purification was then carried out by using an ion exchange resin to obtain 0.45 g and 0.31 g of vistinide, respectively.

Embodiment 3

[0033] Example 3: Method for the production of Villetamide with TFA by using an autoclave

[0034] Put 10 g of pure acarbose into 10% TFA solution to make the final concentration 5%. While raising the pressure using an autoclave at a reaction temperature of 121° C., the system was allowed to react for 30 minutes to 1 hour, followed by removal of TFA and water. Purification was then performed by using an ion exchange resin to obtain 2.1 g of villetamide.

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Abstract

The present invention relates to a method for the preparation of vistilide from acarbose and / or acarbose derivatives using the organic acid TFA (trifluoroacetic acid). Using the method of the present invention, the selective hydrolysis of acarbose and / or acarbose derivatives using TFA produces a large amount of voglibose core which is a strong inhibitor of α-glucosidase and can be used for the treatment of diabetes Precursor, that is, villetamide.

Description

technical field [0001] The present invention relates to a process for the production of valienamine, more particularly, the present invention relates to a process for the production of valienamine at a significantly high conversion rate by the following steps: by using TFA selective hydrolysis from acarbose and and / or acarbose derivatives for the large-scale production of villetamide from which by-products, namely mono-, di-, and tri-saccharides are removed. Background technique [0002] Conventional techniques involved in the commercial production of retidine can be divided into two types. The first type relates to a method of directly producing retaminophen by fermentation using microorganisms, and the second type relates to a method of producing a retidine derivative validamycin through degradation using other microorganisms. [0003] Validamycin derivatives mainly include a valitainide moiety, which is selectively combined with validamine or valid olamine (valiolamine)....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C209/62C07C213/00A61K31/704C07B61/00C07C29/14C07C215/44C07F9/54
CPCC07C213/00C07F9/54C07C2601/10C07C215/44
Inventor 许栗吴振焕
Owner B T GIN · CO LTD
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