High-purity beraprost sodium as well as preparation method and application thereof

A beraprost sodium and high-purity technology, applied in the field of high-purity beraprost sodium and its preparation, can solve the problems of excessive inorganic salts in the product, uncontrollable production process, unstable process and the like, and achieve product stability Good performance, reducing the difficulty of process operation, and mild conditions

Inactive Publication Date: 2013-03-06
SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It can be seen that there are significant defects in the preparation of beraprost sodium (compound of formula 1) in the prior art, the production process is uncontrollable, the process is not stable, the quality cannot be guaranteed, and it is very easy to cause the product to contain excessive inorganic salts, which is not conducive to industrial production requirements

Method used

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  • High-purity beraprost sodium as well as preparation method and application thereof
  • High-purity beraprost sodium as well as preparation method and application thereof
  • High-purity beraprost sodium as well as preparation method and application thereof

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preparation example Construction

[0051] Preparation of Beraprost Sodium

[0052] The preparation method of the high-purity beraprost sodium provided by the invention, said method comprises steps:

[0053] A. loading the solution containing the crude product of beraprost sodium on a macroporous adsorption resin column;

[0054] b. sequentially elute the macroporous adsorption resin column with water and an aqueous solution of an organic solvent, and collect the collection solution containing beraprost sodium;

[0055] c. Concentrating and drying the collected solution to obtain the high-purity beraprost sodium.

[0056] The organic solvent described in step b is selected from one or more of the following solvents: methanol, ethanol, isopropanol, n-propanol, n-butanol, isobutanol, tert-butanol, acetone, butanol Ketones, acetonitrile.

[0057] As used herein, "crude product of beraprost sodium" or "crude product of the compound represented by formula 1" can be used interchangeably. The crude product of the c...

Embodiment 1

[0104] Preparation of compounds of formula 2

[0105] Referring to the method reported in WO03 / 011849 or EP0084856A1, the crude product of the compound of formula 2 was prepared. For the preparation process, see Examples 1 to 7 of WO03 / 011849, or Reference Examples 1 to 8 and Example 1 reported in EP0084856A1 to 2.

Embodiment 2

[0107] Preparation of compounds of formula 3a

[0108]

[0109] Referring to the method reported in WO03 / 011849, the compound of formula 3a was prepared. For the preparation process, see Examples 1 to 5 reported in WO03 / 011849.

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Abstract

The invention discloses high-purity beraprost sodium as well as a preparation method and application thereof. The preparation method of the high-purity beraprost sodium comprises the steps of: desalting a solution containing a beraprost sodium crude product through macroporous resin, then concentrating and drying to obtain the high-purity beraprost sodium with a low inorganic salt content, wherein the mass percent of inorganic salt contained in the high-purity beraprost sodium is less than 0.5 percent. The invention also discloses application of the high-purity beraprost sodium and a medicine composition containing the high-purity beraprost sodium.

Description

technical field [0001] The invention relates to organic compounds, in particular to a high-purity beraprost sodium and its preparation method and application. technical background [0002] In recent years, the incidence of pulmonary hypertension has been rising steadily, and it has gradually become a major category of cardiovascular diseases. [0003] Clinical studies have shown that prostacyclin has a good effect on the treatment of pulmonary arterial hypertension. Currently clinically used prostacyclin drugs include epoprostenol, treprostinil, iloprost, and beraprost sodium. Among them, epoprostenol, treprostinil and iloprost are administered by intravenous injection or inhalation, which is extremely inconvenient for long-term medication. Beraprost sodium is an orally active prostacyclin analogue, which can be rapidly absorbed after oral administration on an empty stomach and is convenient to use, so it has broad application prospects. [0004] At present, there are onl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/93A61K31/5585A61P9/12A61P17/02A61P29/02
Inventor 何兵明唐志军季晓铭
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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