Method of preparing obeticholic acid

A technology of obeticholic acid and intermediates, which is applied in the field of preparation of obeticholic acid intermediates and obeticholic acid, pharmaceutical intermediates, and can solve the problems of increasing the difficulty of feeding and post-processing, increasing production costs, etc. , to achieve the effect of reducing synthesis cost, easy to realize, and good stereoselectivity
CN108250262AInactive Publication Date: 2018-07-06LIVZON NEW NORTH RIVER PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
LIVZON NEW NORTH RIVER PHARMA
Publication Date
2018-07-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method of preparing an obeticholic acid intermediate and obeticholic acid. A synthesis route of the intermediate is shown below as shown in the specification. The preparationmethod has good stereoselectivity in a reaction process, so that the synthesis difficulty of obeticholic acid is greatly reduced, and the synthesis cost of obeticholic acid is lowered. The method ismild in reaction conditions and easy to realize industrially, and the low-impurity obeticholic acid intermediate and obeticholic acid can be obtained. Raw materials used by the method are safe and lowin cost, and the production cost is effectively lowered.
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Description

technical field

[0001] The invention relates to the field of pharmacy, in particular to a synthesis process of a pharmaceutical intermediate, in particular to a method for preparing an obeticholic acid intermediate and obeticholic acid. Background technique

[0002] Obeticholic Acid (Obeticholic Acid, CAS: 459789-99-2), trade name Ocalive, chemical name 3α, 7α-dihydroxy-6α-ethyl-5β-cholanic acid, has a specific three-dimensional structure, and its structural formula is as follows The formula shows:

[0003]

[0004] Obeticholic acid is a new type of drug for the treatment of primary biliary cirrhosis (PBC) developed by the Intercept company of the United States. It was approved on May 27, 2016 and December 12, 2016. It has been approved by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA). Primary biliary cirrhosis (PBC) is a chronic, progressive autoimmune disease, 90% of which occur in women (mostly women aged 40-60). The final conclus...

Claims

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