Process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsBjoern Bartels, Serena Maria Fantasia, Alexander Flohr, Kurt Puentener, Shaoning Wang
Life of this patent
Estimating the term…
Abstract
The invention relates to a novel process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I or of a salt thereof wherein R1 stands for hydrogen, a halogen, for an optionally protected hydroxyl group or for an optionally protected amino group and R2 is hydrogen or a halogen. 2-Phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I with their 1,2,4-triazole nucleus build the structural core of a great number of functionalized molecules in medicinal chemistry.
Claims13
A process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I or of a salt thereof
- wherein,
- R1 stands for hydrogen, a halogen, for an optionally protected hydroxyl group or for an optionally protected amino group and
- R2 is hydrogen or a halogen,
- which comprises the conversion of a pyridine compound of formula II or of a salt thereof,
- wherein, R1 and R2 are as above,
- with benzonitrile in the presence of a Cu-catalyst, a 1,10-phenanthroline derivative and of a mixture O2/N2 , characterized in that no other solvent than the reactant benzonitrile is present in the process.
Dependencies are inferred from the claim text.