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US 8,946,416 B2Granted
Process for the synthesis of 5-(methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzeneamine
AssigneeNovartis AG
InventorsWen-Chung Shieh, Joseph McKenna
Life of this patent
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Abstract
The present invention provides a new method of making compounds of formula (I): wherein R1 is mono- or polysubstituted aryl; R2 is hydrogen, lower alkyl or aryl; and R4 is hydrogen, lower alkyl or halogen.
Claims2
A method for preparing a monohydrochloride salt of 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide of formula:
- comprising the step of reacting a compound of formula
- with 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzenamine wherein the process is catalyzed by a base selected from the group consisting of metal hydride, bulky alkyl lithium metal alkoxide, metal bis(trimethylsilyl)amide, and lithium dialkylamide in an organic solvent.
A method for preparing 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide of formula:
- comprising the step of using a compound of formula:
- with 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzenamine wherein the process is catalyzed by a base selected from the group consisting of metal hydride, bulky alkyl lithium metal alkoxide, metal bis(trimethylsilyl)amide, and lithium dialkylamide in an organic solvent.
Dependencies are inferred from the claim text.