New compound for synthesizing Enzalutamide
2014
The present invention provides a compound Z-M for synthesizing enzalutamide, and a preparation method thereof, wherein R is selected from allyl, propargyl, benzyl, glycidyl or other groups containing alpha and beta unsaturated groups. According to the present invention, with the new series of the compound Z-M, the use of the toxic reagent iodomethane can be avoided during the key intermediate 2-(3-fluoro-4-(methylcarbamoyl)phenylamino)2-methyl methyl propionate preparation, and the conditions of the enzalutamide synthesis Edman degradation reaction of the new intermediate Z-M and an isothiocyanate compound 7 are superior to the reaction conditions of the methyl ester intermediate in the original literature report. The structure of the compound Z-M is defined in the specification.
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