Method for preparing beraprost 314-d sodium

A novel synthesis method for beraprost 314-d sodium achieves high purity and yield without chiral chromatography, addressing inefficiencies in existing methods and ensuring uniformity in formulations, particularly for low-dose applications.

WO2025250828A1 Publication Date: 2025-12-04YS LIFE SCI CO LTD +1
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Patent Information

Application Number
PCT/US2025/031486
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-05-30
Filing Date
2025-05-29
Publication Date
2025-12-04

AI Technical Summary

Technical Problem

Existing synthetic methods for beraprost 314-d sodium are inefficient, require multiple purification steps, and struggle with enantiomeric separation, leading to impure formulations, especially for low-dose applications, which are not commercially viable.

Method used

A method involving a condensation reaction, coupling, hydrolysis, protection, radical cyclization, and trapping steps to produce beraprost 314-d sodium with high purity and yield, avoiding chiral chromatography to achieve high diastereomer purity and enantioselectivity.

Benefits of technology

The method produces beraprost 314-d sodium with at least 90% purity and minimal impurities, ensuring uniformity across dose ranges, particularly for low-dose formulations, and maintains the compound's biological activity.

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Abstract

The present disclosure provides methods of synthesizing a compound of Formula I. The method proceeds through several different pathways including a radical cyclization. Also disclosed are compositions the compound of Formula I as well as methods of using the compound of Formula I in the treatment several conditions or disorders.
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