- Halogen-containing pyrazoleformonitrile derivative synthesis method
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The present invention discloses a halogen-containing pyrazoleformonitrile derivative synthesis method, which comprises that a dialkylacrylonitrile represented by a formula (1) and a carboxylic acid represented by a formula (2) are subjected to an acylation reaction in the presence of a halogenating agent and an organic alkali to obtain 2-acyl-1-aminoacrylonitrile represented by a formula (3), and the 2-acyl-1-aminoacrylonitrile represented by the formula (3) and a substituted hydrazine represented by a formula (4) are subjected to a cyclization reaction under an alkali condition to obtain the pyrazoleformonitrile derivative represented by a formula (5). According to the present invention, with the method, the less coloring 2-acyl-1-aminoacrylonitrile can be synthesized in the high yield manner and the less coloring 1,3-disubstituted pyrazole-4-formonitrile can be synthesized in the high yield and the selectivity manner, and the 1,5-disubstituted pyrazole-4-formonitrile isomer in the product is significantly reduced. The formulas (1)-(5) are defined in the specification.
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Paragraph 0062; 0063; 0064; 0074; 0075; 0076; 0077
(2017/08/28)
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- FLUORINE-CONTAINING PYRAZOLECARBONITRILE DERIVATIVE AND METHOD FOR PRODUCING THE SAME, AND FLUORINE-CONTAINING PYRAZOLECARBOXYLIC ACID DERIVATIVE OBTAINED BY USING THE FLUORINE-CONTAINING PYRAZOLECARBONITRILE DERIVATIVE AND METHOD FOR PRODUCING THE SAME
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The present invention provides a fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same, and a fluorine-containing pyrazolecarboxylic acid derivative obtained by using the fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same. A fluorine-containing acyacrylonitrile derivative prepared from a fluoroacyl derivative and an aminoacrylonitrile derivative, is reacted with a hydrazine derivative to produce a fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1). In Formula (1), Rf represents an alkyl group having 1 to 6 carbon atoms and substituted with at least one fluorine atom; R1 represents an alkyl group having 1 to 6 carbon atoms and R2 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like. The fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1) is reacted with water to produce a fluorine-containing pyrazolecarboxylic acid derivative.
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Page/Page column 29
(2009/12/23)
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