Process for racemizing and isolating the atrop isomer of 7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridine-3-yl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
By heating (P)-compound A at high temperatures and using solvent separation techniques, the process addresses inefficiencies in isolating and reusing (P)-compound A, achieving cost-effective and waste-reducing recovery of (M)-compound A for large-scale synthesis.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- AMGEN INC
- Filing Date
- 2026-02-25
- Publication Date
- 2026-06-09
AI Technical Summary
Existing processes for isolating and reusing the (P)-isomer of compound A, a synthetic intermediate in the synthesis of AMG 510, are inefficient, costly, and generate significant waste due to low yields and high energy barriers, making them impractical for large-scale operations.
A method involving heating a composition of (P)-compound A or its salt with a solvent at high temperatures (250°C to 350°C) to racemize it, followed by a process to isolate and reuse (P)-compound A, including the use of bases to separate tartrate salts and solvents, allowing for efficient recovery and regeneration of (M)-compound A.
The process significantly reduces waste and costs by enabling the efficient recovery of (M)-compound A from what was previously considered wastewater, improving the overall efficiency and reducing the number of batches required, while maintaining low impurity levels.
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