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US 12,466,825 B2Granted
Synthesis of KRAS G12C inhibitor compound
AssigneeAmgen Inc.
InventorsAndrew T. Parsons, Matthew Beaver
Life of this patent
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Abstract
The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2,2′,2″-(1,3,5,2,4,6-trioxatriborinane-2,4,6-triyl)tris(3-fluorophenol), useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
Claims42
A compound of Formula 6A:
A composition, the composition comprising a compound of Formula 6A:
A method of making a compound of Formula 6A:
- the method comprising reacting a mixture comprising a compound having the structure:
- with an acid with at least one solvent.
A process of preparing a compound of Formula 6A:
- comprising admixing (2-fluoro-6-methoxyphenyl) boronic acid with BBr3 in at least one solvent to provide the compound of Formula 6A.
A process of preparing a compound of Formula 7
- comprising admixing a compound of Formula 6A:
- with a compound of Formula 6:
- in the presence of a catalyst and potassium acetate to form the compound of Formula (7).
Dependencies are inferred from the claim text.