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Compound for preparing fondaparinux sodium, preparation method thereof and preparation method of fondaparinux sodium

A compound and stereochemical technology, applied in the production of sugar derivatives, organic chemistry, bulk chemicals, etc., can solve the problems of low yield and complicated steps of fondaparinux

Active Publication Date: 2013-05-29
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a result, it has directly caused the complex steps of synthesizing fondaparinux sodium from the initial raw material, and the yield is low

Method used

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  • Compound for preparing fondaparinux sodium, preparation method thereof and preparation method of fondaparinux sodium
  • Compound for preparing fondaparinux sodium, preparation method thereof and preparation method of fondaparinux sodium
  • Compound for preparing fondaparinux sodium, preparation method thereof and preparation method of fondaparinux sodium

Examples

Experimental program
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Effect test

Embodiment 1

[0086]

[0087] Heat 8.5g (2.95mmol) of phosphotungstic acid at 80°C for 0.5h under vacuum of 4 mm Hg, cool down naturally to 40°C under vacuum, and pass through N 2, add 2.5g (5.8mmol) GBn (can use Carbohydrate Research 2003, 338, 681-686 shown synthetic compound 6 similar method to prepare) and 3g (7.3mmol) HBz (can use Angew.Chem.Int.Ed .Engl.1993.32.1671-1690 page 1674~1675 shown in the synthetic compound 10a similar method to be prepared), anhydrous and anaerobic operation, N 2 50ml of toluene was added under low temperature, the temperature was lowered to -5°C, 0.2ml (1.1mmol) of TMSOTf was added, and kept at 0°C for 3h, then kept at + ].

Embodiment 2

[0089] Heat 3.3g of phosphotungstic acid at 80°C and 4mm Hg vacuum for 0.5h, then naturally cool down to 40°C under vacuum, and pass through N 2 , add 2.5g (5.8mmol) GBn and 3g (7.3mmol) HBz, anhydrous and anaerobic operation, N 2 Add 50ml of toluene at low temperature, cool down to -5°C, add 0.31ml of TMSOTf, keep at 0°C for 3h, then keep the temperature + ].

Embodiment 3

[0091] N 2 2.5gGBn and 3gHBz were dissolved in 50ml of dichloromethane, cooled to -5°C, TMSOTf 0.7ml (3.8mmol) was added, kept at 0°C for 3h, then kept at + ].

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Abstract

The invention relates to a compound as shown in formula I for preparing fondaparinux sodium, a preparation method thereof and a preparation method of the fondaparinux sodium. The compound disclosed by the invention can be prepared from raw materials which are easy to obtain at higher selectivity and yield, thereby greatly simplifying the preparation process of the fondaparinux sodium. The definition of various substitutional groups contained in the formula I is the same as the definition in a specification.

Description

technical field [0001] The invention relates to a compound used for preparing fondaparinux sodium, a preparation method thereof and a method for preparing fondaparinux sodium. Background technique [0002] Fondaparinux sodium (Fondaparin, Fondaparinux sodium), its structure is as follows, the five sugar rings are named D, E, F, G, H rings from left to right according to the custom. [0003] [0004] It is a highly selective factor Xa inhibitor developed by Sanofi, France, and later transferred to GlaxoSmithKline (GSK). It was launched in Europe in 2001, in the United States in 2002, and in China in 2008. It's called "Android". It is obtained by chemical synthesis, a single compound with a definite structure and a definite molecular weight. It is currently the most efficient and highly selective factor Xa inhibitor. Unlike enoxaparin, nadroparin and other low-molecular-weight heparins derived from animals, fondaparinux sodium is a pure substance with a single structure,...

Claims

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Application Information

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IPC IPC(8): C07H15/04
CPCY02P20/55
Inventor 林峰姜浩朱晓峰陈建丽卢锐钟稼义
Owner JIANGSU HENGRUI MEDICINE CO LTD
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