METHOD FOR PREPARING TELAPREVIR AND INTERMEDIATE THEREOF

摘要

Disclosed is a method for preparing telaprevir and an intermediate thereof. The intermediate disclosed in the present invention is the formula-I compound or the acidic salt of the compound, and is prepared by condensing the formula-III compound and the formula-IV compound; and the obtained intermediate further reacts with the formula-A compound to obtain telaprevir. In the formula, the definition of R1 is as described in the specification. In the method of the present invention, the raw materials are simple and easy to obtain, the reaction condition is moderate, and the last-step oxidation reaction in the prior art is avoided, thereby greatly improving the total yield. Therefore, the method is applicable to industrial applications.