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Preparation method for monosaccharide fragment intermediate of fondaparinux sodium as anticoagulant drug

A fondaparinux sodium and intermediate technology is applied in the field of preparation of an anticoagulant drug fondaparinux sodium monosaccharide fragment A intermediate, and can solve the problems of difficulty in realizing industrialized production, efficient separation, low overall synthesis efficiency and the like , to achieve the effect of solving technical bottlenecks

Active Publication Date: 2015-12-23
CHONGQING UNIV
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Problems solved by technology

For the preparation of its A fragment, the current technical bottleneck is mainly reflected in the difficulty in efficiently separating its α and β-isomers during the process of introducing the 1-methoxy group, usually by recrystallization or multi-step Chemical transformation to achieve the above purpose (US4818816, US20050080042; CN103122012; Hung, S.-C.Angew.Chem.Int.Ed.2014,53,9876; Shen, J.; Zhao, W.; Wang, P.etal. Chem.Med.Chem.2014,9,1071), but the existing methods have the defects of low overall synthesis efficiency and difficulty in realizing industrial production to varying degrees

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  • Preparation method for monosaccharide fragment intermediate of fondaparinux sodium as anticoagulant drug
  • Preparation method for monosaccharide fragment intermediate of fondaparinux sodium as anticoagulant drug
  • Preparation method for monosaccharide fragment intermediate of fondaparinux sodium as anticoagulant drug

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Embodiment Construction

[0028] The embodiment of the present invention discloses a method for preparing a single optically active fondaparinux sodium fragment A. Those skilled in the art can refer to the content of this article to appropriately improve the process parameters to achieve. In particular, it should be pointed out that all similar replacements and modifications are obvious to those skilled in the art, and they are all considered to be included in the present invention. The method of the present invention has been described through preferred embodiments, and relevant personnel can obviously make changes or appropriate changes and combinations to the method described herein without departing from the content, spirit and scope of the present invention to realize and apply the technology of the present invention .

[0029] In order to further understand the present invention, the present invention will be described in detail below in conjunction with examples.

[0030] The preparation of co...

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Abstract

The invention provides a preparation method for a monosaccharide fragment intermediate of fondaparinux sodium as an anticoagulant drug, and the intermediate can be used in the preparation of the fondaparinux sodium as the anticoagulant drug. The method is easy to operate, can realize the kilogram-level preparation of fondaparinux sodium monosaccharide fragment A intermediate with single-optical activity, solves the technical bottleneck of conventional fondaparinux sodium fragment A synthesis, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicine and chemical industry, in particular to a preparation method of an anticoagulant drug fondaparinux sodium monosaccharide fragment A intermediate. Background technique [0002] Thrombotic disease is one of the major diseases with the highest incidence rate in modern society. Among them, venous thrombosis induced by surgery, trauma (such as large-scale or lower extremity trauma), acute medical diseases (such as myocardial infarction, stroke), cancer treatment (such as hormone therapy, chemotherapy, radiotherapy), etc. Cardiopulmonary syndrome and the third major cardiovascular disease after stroke, which seriously threaten human health. At present, the prevention and treatment of venous thrombosis mainly focus on anticoagulation. Traditional anticoagulant drugs represented by unfractionated heparin and warfarin have been gradually replaced by a new generation of anticoagulant drugs due to various degrees o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/04C07H1/00
Inventor 秦勇唐培杨超戴翔王树青
Owner CHONGQING UNIV
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