Preparation of biaryl compounds

C - Chemistry – Metallurgy – 07 – C

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260/478.5, 260/5

C07C 69/65 (2006.01) B01J 27/122 (2006.01) C07B 37/06 (2006.01) C07C 69/616 (2006.01)

Patent

CA 1209159

ABSTRACT PREPARATION OF BIARYL COMPOUNDS Biaryl compounds are prepared by coupling an arylamine with an aromatic compound in the presence of an alkyl nitrite and 0.04-0.6 mol of an acid having a dissociation constant of at least 1.7 x 10-5 at 25°C. and about 0.08-1.3 mols of a cuprous halide catalyst per mol of the arylamine. The invention has particular utility in the coupling with aromatic compounds of arylamines having acid-sensitive ar-substituents, e.g. flurbiprofen intermediates, such as 2-(4-amino-3- fluorobenzene)propionitrile and alkyl 2-(4-amino-3- fluorobenzene)propionates.

452610

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