Estrogen receptor degrading agent intermediates and preparation method therefor
WO2026138908A1PCT designated stage Publication Date: 2026-07-02HINOVA PHARM INC
Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- HINOVA PHARM INC
- Filing Date
- 2025-12-24
- Publication Date
- 2026-07-02
AI Technical Summary
Technical Problem
Existing synthetic routes for estrogen receptor degraders and their intermediates are lengthy and have low yields, limiting their large-scale industrial production.
Method used
A novel synthetic method is employed to prepare compounds of formula I, II, or IV via reactions 1 to 5, including the use of organophosphorus reagents, azodicarboxylic esters, transition metal catalysts, and bases, with optimized reaction conditions to improve synthetic efficiency.
Benefits of technology
It shortens the synthesis route, increases the yield, and is suitable for large-scale industrial production.
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Smart Images
Figure PCTCN2025145309-FTAPPB-I100001 
Figure PCTCN2025145309-FTAPPB-I100002 
Figure PCTCN2025145309-FTAPPB-I100003
Abstract
The present invention relates to the technical field of medical synthesis, and provides a series of compounds as synthetic intermediates to construct a novel method for synthesizing estrogen receptor degrading agent intermediates. The synthesis method has a short route and a high yield.
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