Method for producing substituted biphenyls

C - Chemistry – Metallurgy – 07 – C

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C07C 205/11 (2006.01) C07C 205/12 (2006.01)

Patent

CA 2727075

The invention relates to a method for producing substituted biphenyls of formula (I), wherein R1 = nitro or amino, R2 = cyano, halide, C1- C4 alkyl halide, C1-C4 alkoxy halide or C1-C4 alkylthio halide, n = 0 to 3 and R3 = hydrogen, cyano or halide, characterized by reacting a halobenzene of formula (I1), wherein HaI represents chlorine or bromine, with a phenyl boronic acid (IVa) of a diphenyl borinic acid (IVb) or a mixture of (IVa) and (IVb) in a solvent or diluent in the presence of a base and of a palladium catalyst which consists of palladium and a bidentate phosphorus ligand of formula (III), wherein Ar represents optionally substituted phenyl and R4 and R5 represent C1-C8 alkyl or C3-C6 cycloalkyl each or together form a two- to seven-membered bridge which can optionally carry a C1-C6 alkyl substituent.

L'invention concerne un procédé de fabrication de biphényles substitués représentés par la formule générale (I) dans laquelle R1 = nitro ou amino, R2 = cyano, halogène, C1-C4-halogénoalkyle, C1-C4-halogénoalkoxy ou C1-C4-halogénoalkylthio, n = 0 à 3 et R3 = hydrogène, cyano ou halogène. Le procédé est caractérisé en ce qu'il consiste à faire réagir un halogénobenzole représenté par la formule (II) dans laquelle Hal est chlore ou brome, en présence d'une base et d'un catalyseur au palladium composé de palladium et d'un ligand phosphoré bidenté représenté par la formule (III) dans laquelle Ar est phényle éventuellement substitué et R4 et R5 sont respectivement C1-C8-alkyle ou C3-C6-cycloalkyle ou forment ensemble un pont à 2 à 7 éléments pouvant éventuellement porter un substituant C1-C6-alkyle, dans un solvant ou un diluant, avec un acide phénylborique (IVa), un acide diphénylborique (IVb) ou un mélange de (IVa) et (IVb).

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