Process for preparing antiviral agent
By employing a multi-step synthesis method and chiral resolution technology, the problem of low purity in the preparation of entecavir was solved, and the preparation of high-purity entecavir was achieved.
CN104788485AInactive Publication Date: 2015-07-22BRISTOL MYERS SQUIBB HLDG IRELAND UNLTD
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Patent Information
- Application Number
- CN201510061020.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2002-12-11
- Filing Date
- 2003-12-10
- Publication Date
- 2015-07-22
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
Technical Problem
Existing methods for preparing entecavir suffer from low enantiomeric and diastereomeric purity, making it difficult to meet the demand for high-purity entecavir.
Method used
A multi-step synthetic method was adopted, including ester preparation, epoxidation and reduction, coupling reaction, etc., and chiral amine resolution, resin adsorption and other techniques were used to achieve the preparation of high-purity entecavir.
Benefits of technology
High diastereomeric and enantiomeric purity of entecavir was achieved, improving the efficiency of the preparation process and the purity of the product.
✦ Generated by Eureka AI based on patent content.
Abstract
The invention refers to a method for isolating entecavir or an entecavir intermediate from a diluted mixture, the diluted mixture comprising entecavir and water or a mixture comprising an entecavir intermediate and other process reagents comprising: (a) adsorbing the diluted mixture onto a hydrophobic resin bed; (b) washing the resin bed with water to remove salt; and (c) eluting the entecavir or entecavir intermediate from the resin bed with an organic solvent.
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