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Intermediate for preparing fondaparinux sodium, preparation method thereof, and fondaparinux sodium preparation method

A technology of benzyl group and protecting group, applied in the field of preparing fondaparinux sodium, can solve problems such as low yield, complicated steps of fondaparinux sodium and the like

Active Publication Date: 2015-12-09
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, the steps of synthesizing fondaparinux sodium from the initial raw material are directly complicated and the yield is low

Method used

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  • Intermediate for preparing fondaparinux sodium, preparation method thereof, and fondaparinux sodium preparation method
  • Intermediate for preparing fondaparinux sodium, preparation method thereof, and fondaparinux sodium preparation method
  • Intermediate for preparing fondaparinux sodium, preparation method thereof, and fondaparinux sodium preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087]

[0088] 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 be prepared using the method similar to the synthetic compound 6 shown in CarbohydrateResearch2003,338,681-686) and 3g (7.3mmol) HBz (can be used 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 Add 50ml of toluene at low temperature, cool down to -5°C, add TMSOTf 0.2ml (1.1mmol), keep at 0°C for 3h, then keep the temperature + ].

Embodiment 2

[0090] 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

[0092] 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

[0001] This application is a Chinese patent application with the application number 201110405005.9, the application date is December 8, 2011, and the invention title is "compounds for preparing fondaparinux sodium and its preparation method, and preparation method of fondaparinux sodium" divisional application. technical field [0002] The invention relates to a compound used for preparing fondaparinux sodium, a preparation method thereof and a method for preparing fondaparinux sodium. Background technique [0003] The structure of Fondaparinux sodium (Fondaparin, Fondaparinuxsodium) is as follows, and the five sugar rings are named D, E, F, G, and H rings from left to right according to the habit. [0004] [0005] 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/04C07H1/00
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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