Copper catalyzed arylation
OwnerFrederick Hicksinventor
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Abstract
The present invention is directed to an arylation of a nuclophile by reacting the nucleophile with a substrate aromatic compound ArX in the presence of a copper catalyst, a base and water, wherein Ar is aryl, heteroaryl or alkenyl, X is halo, sulfonate or phosphonate, the base comprises an alkaline earth carbonate, bicarbonate, hydroxide or phosphate, and the copper catalyst comprises a copper atom or ion and a ligand.
Claims20
A method for arylating a nuclophile, comprising reacting the nucleophile with a substrate aromatic compound, ArX, in the presence of a copper catalyst, a base and water, wherein Ar is aryl, heteroaryl or alkenyl, X is halo, sulfonate or phosphonate, the base comprises an alkaline earth carbonate, bicarbonate, hydroxide or phosphate, and the copper catalyst comprises a copper atom or ion and a ligand.
A method for arylating a HN-containing heterocycle, comprising reacting the HN-containing heterocycle with a substrate aromatic compound, ArX, according to the reaction scheme:
- wherein Ar is aryl, heteroaryl or alkenyl,
- X is halo, sulfonate or phosphonate,
- the base comprises an alkaline earth carbonate, bicarbonate, hydroxide or phosphate, and
- the copper catalyst comprises a copper atom or ion and a ligand.
A method for arylating a HN-containing compound according to the formula HN(R1)R2, comprising reacting the HN-containing compound with a substrate aromatic compound, ArX, according to the reaction scheme:
- wherein Ar is aryl, heteroaryl or alkenyl,
- X is halo, sulfonate or phosphonate
- R1 is H, alkyl or aryl
- R2 is according to the formula:
- wherein R3 is H, alkyl, aryl, heteroaryl, alkenyl, —OR5 or —NR62, and R5 and R6 are each independently alkyl, aryl, or
- wherein R7 is alkyl or aryl,
- the base comprises an alkaline earth carbonate, bicarbonate, hydroxide or phosphate, and
- the copper catalyst comprises a copper atom or ion and a ligand.
Dependencies are inferred from the claim text.