Process for the preparation of 3-substituted 5-amino-6h-thiazolo[4,5-d]pyrimidine-2,7-dione compounds
Patent Information
- Authority / Receiving Office
- EP · EP
- Patent Type
- Applications
- Current Assignee / Owner
- F HOFFMANN LA ROCHE & CO AG
- Filing Date
- 2024-08-06
- Publication Date
- 2026-06-17
AI Technical Summary
Existing processes for manufacturing 3-substituted 5-amino-6/7-thiazolo[4,5-rf]pyrimidine-2,7-dione compounds suffer from low purity and yield due to harsh reaction conditions, low selectivity, and the need for additional purification steps.
A process involving specific reaction steps such as reacting a compound of formula (VIII) with a Grignard reagent in the presence of a copper catalyst, followed by acylating agents and silylating agents, to form compound (XIII), which is then reacted with an acid and an aqueous base to achieve compound (la) with improved purity and yield.
The proposed process enhances the purity and yield of the compound (la), allowing for its isolation in the free form in high purity and simplifying the manufacturing process, making it more suitable for large-scale production.
Smart Images
Figure EP2024072228_13022025_PF_FP_ABST