- Imidazole acetonitrile derivative acid salt as well as preparation method and application thereof
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The invention relates to an imidazole acetonitrile derivative acid salt as well as a preparation method and an application thereof, belongs to the technical field of drug synthesis, and aims to solve the problem about how to improve stability and increase the yield. The method comprises steps as follows: an imidazole acetonitrile derivative is dissolved in a water-insoluble polar organic solvent, then corresponding acid is added for a salt forming reaction, and the acid salt of the product imidazole acetonitrile derivative is gradually separated out, and applied to preparation of Luliconazole. The acid salt itself has better stability and used as an intermediate for preparing Luliconazole at the same time, the problem of mutual inversion of Z-E configuration in the Luliconazole preparation process can be solved, the Z configuration can be inverted into the E configuration, the configuration inversion stability is guaranteed, and the yield is higher. The effects of simple technology and easiness in operation are also realized.
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Paragraph 0100; 0101
(2016/10/10)
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- Method for synthesizing Luliconazole
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The invention relates to a method for synthesizing Luliconazole. The method comprises the steps of subjecting m-dichlorobenzene to Friedel-Crafts acylation with chloroacetyl chloride, catalytic chiral reduction with (S)-2-methyl-CBS-oxazaborolidine and esterification with methylsulfonyl chloride so as to obtain (S)-2,2',4'-ethyl trichlorobenzene methanesulfonate, and finally, subjecting (S)-2,2',4'-ethyl trichlorobenzene methanesulfonate to a reaction with carbon disulfide and imidazolyl acetonitrile, thereby obtaining Luliconazole. According to the method, the total yield is about 30%.
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- EXTERNAL PHARMACEUTICAL COMPOSITION
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A pharmaceutical composition for external use, including: i) luliconazole represented by the following structural formula (1) and/or a salt thereof; and ii) one or two or more selected from N-methyl-2-pyrrolidone, propylene carbonate, and crotamiton.
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Page/Page column 7-8
(2009/01/24)
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