Process for the arylation of aza-heterocycles with activated...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/08 (2006.01) C07C 205/37 (2006.01) C07C 205/56 (2006.01) C07C 209/10 (2006.01) C07C 211/52 (2006.01) C07C 213/06 (2006.01) C07C 217/20 (2006.01) C07C 381/10 (2006.01) C07D 207/32 (2006.01) C07D 209/12 (2006.01) C07D 209/42 (2006.01) C07D 209/86 (2006.01) C07D 231/56 (2006.01) C07D 233/60 (2006.01) C07D 235/06 (2006.01) C07D 249/06 (2006.01) C07D 249/08 (2006.01) C07D 249/20 (2006.01) C07D 295/08 (2006.01) C07D 295/092 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2360923

The invention relates to a method for producing N-aryl-aza-heterocycles of general formula (I) in which: R1, R2, R3, R4 and R5 are the same or different and represent a hydrogen atom, a nitro group, a cyano group, an alkoxycarbonyl group with up to 5 C atoms, an aldehyde group, an alkylcarbonyl group with up to 5 C atoms, an arylcarbonyl group or an amide group, whereby the radicals R1 to R5 can not all be a hydrogen atom at the same time, and; HETN represents an aromatic aza-heterocycle with 5 or 6 ring atoms, whereby up to 3 ring atoms can be nitrogen atoms, and up to two additional aromatic carbon rings can be fused to the heterocycle. The inventive N-aryl-aza-heterocycles are produced by reacting, at room temperature, aza-heterocycles with activated aromatic compounds of general formula (XIV), in which HAL represents a halogen atom, while using cesium carbonate and without adding additional catalysts.

L'invention concerne un procédé qui permet de produire des N-aryl-aza-hétérocycles de formule générale (I). Le procédé consiste à faire réagir des aza-hétérocycles avec des aryl-halogénures activés en présence de carbonate de césium, sans adjonction d'autres catalyseurs et à température ambiante.

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