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Method for preparing 3,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate

A technology of trimethylsilyloxy and trimethylchlorosilane, which is applied in the field of medicine and can solve problems such as increasing difficulties and costs

Active Publication Date: 2016-12-28
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, since triethylamine needs to be used in the reaction of step 2, and triethylamine needs to be removed by extraction after the reaction, water will be introduced into the reaction system, therefore, the reaction system needs to be dehydrated before proceeding Step 3, thus increasing operational difficulties and costs

Method used

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  • Method for preparing 3,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate
  • Method for preparing 3,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate
  • Method for preparing 3,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate

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Embodiment Construction

[0191] Embodiments of the present invention will be described in detail below in conjunction with the drawings and examples, but those skilled in the art will understand that the following drawings and examples are only for illustrating the present invention, and should not be considered as limiting the scope of the present invention. Those who do not indicate the specific conditions in the accompanying drawings and the examples are carried out according to the conventional conditions or the conditions suggested by the manufacturer. The reagents or instruments used were not indicated by the manufacturer, and they were all commercially available conventional products. All anhydrous solvents used are commercially available.

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Abstract

The invention belongs to the technical field of medicines, and relates to a method for preparing 3,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate. Preferentially, 3,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate is 3 alpha,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate. According to the method, 3,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate, especially 3 alpha,7-bis(trimethylsilyl oxyl)-6-alkene-5 beta-cholane-24-methyl gallate, prepared through the method can be used for preparing obeticholic acid.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a method for preparing 3,7-bis(trimethylsilyloxy)-6-en-5β-cholan-24-acid methyl ester, preferably, the 3, 7-bis(trimethylsilyloxy)-6-ene-5β-cholane-24-oic acid methyl ester is 3α,7-bis(trimethylsilyloxy)-6-ene-5β-chol Alkane-24-oic acid methyl ester. 3,7-bis(trimethylsilyloxy)-6-ene-5β-cholane-24-oic acid methyl ester prepared by the method of the present invention, especially 3α,7-bis(trimethylsilyl Oxy)-6-ene-5β-cholane-24-acid methyl ester, which can be used in the preparation of obeticholic acid. Background technique [0002] Farnesoid X receptor (FXR) belongs to the family of ligand-activated transcription factor nuclear receptors, and its natural ligands include primary bile acid chenodeoxycholic acid, secondary bile acid lithocholic acid and deoxycholic acid, etc. FXR is a bile sensor, and its functions include coordinating with other nuclear receptors and participating ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J9/00
CPCC07J9/005
Inventor 李松李行舟钟武郑志兵肖军海周辛波谢云德王晓奎谢菲
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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