- One-pot preparation technology of NS5A protein inhibitor daclatasvir
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The invention discloses a one-pot preparation technology of an NS5A protein inhibitor daclatasvir. The technology mainly comprises the following three steps: 1) preparing an intermediate DT1: carryingout a butt reaction on reaction initial raw materials which are DTM1, DTM2 and DTM3 under the action of an alkali reagent and a condensing agent to prepare the intermediate DT1; 2) preparing an intermediate DT2: cyclizing the intermediate DT1 and an amine compound to prepare the intermediate DT2; and 3) preparing daclatasvir: removing an amino protecting group from the intermediate DT2 by using an amino protecting group removing reagent to prepare the product daclatasvir. The method for preparing daclatasvir has the characteristics of high product yield, simple and easy-to-operate overall process, no strong corrosive substances in the preparation materials, effectiveness in safety ensuring, and suitableness for large-scale industrial production.
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- Preparation method for daclatasvir
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The invention discloses a preparation method for daclatasvir. The preparation method comprises the following steps: in a solvent, performing a cyclization reaction on a compound shown as a formula D10 and ammonium acetate, so as to prepare the daclatasvir shown as a formula I, wherein the cyclization reaction is shown in the description. The preparation method for daclatasvir is low in cost, high in yield, friendly to environment, simple in steps, mild in reaction conditions and suitable for industrialized production.
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Paragraph 0108; 0109; 0132; 0133; 0134; 0135; 0136-0139
(2017/10/22)
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