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Xtandi synthesis method

2014 
The present invention discloses a Xtandi synthesis method, which comprises: carrying out esterification on 2-(3-fluoro-4-methylcarbamoylphenylamino)-2-methyl propionic acid; directly carrying out a reaction at a room temperature for 4-6 h by adopting the 2-(3-fluoro-4-methylcarbamoylphenylamino)-2-methyl propionic acid as a raw material, adopting triethylamine as an acid binding agent, adopting 1-(3-dimethylaminopropyl)-3-ethyl carbodiimide hydrochloride as a condensing agent, adopting 1-hydroxybenzotriazole as a catalyst, and adopting methanol or ethanol as a reactant and solvent; and after completing the reaction, evaporating to remove methanol or ethanol, adding water, stirring, filtering to obtain a filter cake, and carrying out water washing and vacuum drying to obtain 2-(3-fluoro-4-methylcarbamoylphenylamino)-2-methyl methyl propionate or 2-(3-fluoro-4-methylcarbamoylphenylamino)-2-methyl ethyl propionate. The synthesis method has advantages of easily available raw materials, mild reaction conditions, simple operation and post-treatment, safe and nontoxic condensing agent and catalyst, and high product yield.
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