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AssigneeHoffmann-La Roche Inc.
InventorsGuocai Zhang, Weichun Chen
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The present disclosure provides a process for preparing 2-bromo-4-(3,5-difluorophenyl)-4,5,6,7-tetrahydro-5H-[1,2,4]triazolo[1,5-a]pyrimidine. In one example, a corresponding precursor compound is reacted with triphenylphosphine and an azodicarboxylate reagent in an organic solvent at a reduced temperature to form the desired triazolopyrimidine compound. The reaction mixture is quenched with water and extracted with an organic solvent. The combined organic layers are washed with an aqueous salt solution, dried, and concentrated. The resulting residue is treated with an alcohol solvent, and the solid is isolated by filtration. The isolated material is further treated with an ester solvent at an elevated temperature, cooled, isolated by filtration, and dried to provide 2-bromo-4-(3,5-difluorophenyl)-4,5,6,7-tetrahydro-5H-[1,2,4]triazolo[1,5-a]pyrimidine.
A process for the preparation of a compound of formula (VIII):
Dependencies are inferred from the claim text.