Method for producing (6R,10S)-10-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6H)-pyrimidinyl}-1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(methano)pyrazolo[4,3-B][1,7]diazacyclotetradecine-5(6H)-one
A novel method for producing factor XIa inhibitors addresses scaling challenges by using fewer steps and inexpensive materials, achieving high yields suitable for industrial-scale production.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- BRISTOL MYERS SQUIBB CO
- Filing Date
- 2026-04-01
- Publication Date
- 2026-07-07
AI Technical Summary
Existing methods for producing factor XIa inhibitors, such as those disclosed in U.S. Patent No. 9,453,018, face challenges in scaling up synthesis due to high costs of reagents and the need for higher yields, making them unsuitable for industrial-scale production.
A novel method involving fewer synthesis steps and using inexpensive starting materials to produce (6R,10S)-10-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazole-1-yl)phenyl]-6-oxo-1(6H)-pyrimidinyl}-1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(methano)pyrazolo[4,3-b][1,7]diazacyclotetradecine-5(6H)-one, characterized by specific reaction steps and solvate formation, including the use of solvents and reagents like N,N-dimethylformamide dimethylacetal and acetic acid, to achieve high yields.
The method enables the production of higher yields of the factor XIa inhibitor suitable for industrial-scale synthesis, reducing costs and improving manufacturing efficiency.
Smart Images
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