Method for manufacturing a boronic acid ester compound

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 5/02 (2006.01)

Patent

CA 2750353

The present invention relates to a method for manufacturing a boronic acid ester compound, characterized by react-ing an aryl halide compound and a diboron ester compound in the presence of a nitrogen-containing organic base, a nickel cata-lyst, a phosphine compound and a solvent. According to the manufacturing method of the present invention, even if a nickel cata-lyst is used as the catalyst, a desired boronic acid ester compound can be obtained in a sufficiently high yield. Furthermore, even if aryl chloride or aryl bromide having relatively low price and low reactivity, was used as the aryl halide compound, a desired boronic acid ester compound can be obtained in a sufficiently high yield.

La présente invention porte sur un procédé pour la fabrication d'un composé ester de l'acide boronique, caractérisé par la réaction d'un composé halogénure d'aryle et d'un composé ester de dibore en présence d'une base organique contenant de l'azote, d'un catalyseur au nickel, d'un composé phosphine et d'un solvant. Selon le procédé de fabrication de la présente invention, même si un catalyseur au nickel est utilisé comme catalyseur, un composé ester de l'acide boronique souhaité peut être obtenu avec un rendement de production suffisamment élevé. En outre, même si un chlorure d'aryle ou un bromure d'aryle ayant un prix relativement faible et une réactivité relativement faible était utilisé comme composé halogénure d'aryle, un composé ester de l'acide boronique souhaité pourrait être obtenu avec un rendement de production suffisamment élevé.

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