Preparation method of rilpivirine
2016
The invention discloses a preparation method of rilpivirine. The method comprises the following steps: with the compounds of formulas I, II, V and VI as initial raw materials, performing a Heck reaction between the compounds of formulas I and II under the effects of a catalyst, a ligand and alkali, and dehydrating and forming hydrochloride to obtain a key intermediate 1; performing substitution and chlorination of the compounds of formulas V and VI to obtain a key intermediate 2; and performing a microwave-assisted substitution reaction between the intermediate 1 and the intermediate 2 to obtain rilpivirine 3. The preparation method disclosed by the invention has high reaction selectivity and is easy in operation; and compared with original synthesis method, the reaction time is greatly shortened, the energy consumption is reduced, the reaction yield is increased, total yield is as high as 21.4%, and the method is suitable for industrial production.
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