Intermidiate for preparing 1,2-oxygen nitrogen heterocyclic-2-alkene acylbenzene and its preparation

制备1,2-氧氮杂环戊-2-烯基酰基苯用的中间体和其制备

Abstract

描述了用于制备结构式XV和XIX化合物的工艺,以及也描述了利用此工艺进一步制备结构式IX和X化合物的工艺。
Preparation of 4-(4-alkylsulfonyl-3-isoxazolyl- benzoyl)-5-hydroxypyrazole derivatives (I) involves reacting a hydroxypyrazole (II) with a bromobenzene (III) in presence of carbon monoxide, a palladium catalyst, a potassium salt and an amine. Preparation of benzoylpyrazole derivatives of formula (I) comprises reacting a hydroxypyrazole compound of formula (II) with a bromobenzene of formula (III)in the presence of carbon monoxide, a palladium catalyst, one or more equivalents of a potassium salt and one or more equivalents of a tertiary amine of formula N(Ra)3 (IV). Reaction is at 0-40 kg/cm<2> and 100-140 deg C. R<1>, R<4> = 1-4C alkyl; R<2> = Cl or CH3; R<3> = H or 1-4C alkyl; M = H or alkali metal; Ra = 1-6C alkyl, or one can be phenyl or naphthyl; the isoxazole or isoxazoline residueis bonded in the 3- or 5-position.

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Patent Citations (1)

    Publication numberPublication dateAssigneeTitle
    WO-9611906-A1April 25, 1996Novartis AgProcede de preparation de 3-aminobenzonitriles substitues

NO-Patent Citations (3)

    Title
    CHOO S GIMA, ET AL..A SIMPLE PREPARATION OF AROMATIC ORHETEROAROMATIC SULPHIDES.JOURNAL OF THE CHEMICAL SOCIETY, CHEMICAL COMMUNICATIONS.1980,756-757.
    JAMES D. BALEJA.THE FACILE CONVERSION OF AROMATIC AMINES TOARYLMETHYLSULFIDES WITH METHYLTHIOCOPPER.SYNTHETIC COMMUNICATIONS14 3.1984,14(3),215-218.
    SHIGERUOAK ET AL..DIRECT CONVERSION OF ARYLAMINES TO THECORRESPONDING HALIDES

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