- Method for preparing NS5A inhibitor-Velpatasvir
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The invention discloses a method for preparing an NS5A inhibitor-Velpatasvir, wherein the method mainly comprises the five steps: 1) carrying out docking reaction on reaction initial raw materials VPM1, VPM2 and VPM3 under the catalytic action of alkali to prepare an intermediate VP1; 2) removing amino protecting groups from the intermediate VP1 by using a protecting group removing reagent to prepare an intermediate VP2; 3) carrying out cyclization on the intermediate VP2 and an amine compound to prepare an intermediate VP3; 4) carrying out a reaction on the intermediate VP3 with VPM4 under the action of a condensing agent to prepare an amide compound intermediate VP4; and 5) carrying out oxidation reaction on the intermediate VP4 under the action of an oxidizing agent to prepare Velpatasvir. The preparation process of Velpatasvir has the characteristics of simplified route, simple reaction conditions, enhanced operability and higher product yield, and is more suitable for large-scaleindustrial production.
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- His wei uygur handkerchief, intermediate and preparation method (by machine translation)
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The invention discloses uygur handkerchief his wei, intermediate and its preparation method. The invention provides a uygur handkerchief he vee 1 of preparation method, comprises the following steps: in the organic solvent, alkali, catalyst and the presence of a condensing agent, the compound 3 with the MOC - L - valine to carry out the condensation reaction, to obtain uygur handkerchief he vee 1. Preparation method of this invention mild reaction conditions, simple and safe operation, without special purification equipment, avoids the post processing in the course of the operation of the column chromatography separation, the chiral isomer is easy to control, high yield, wei huaxue uygur handkerchief he made and optical purity is greater than 99.50%, all impurity is less than 0.10%, can reach the bulk drug standard, low cost, and is suitable for industrial production. (by machine translation)
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Paragraph 0268-0270
(2018/03/01)
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- Compound used for inhibiting hepatitis C virus, and pharmaceutical applications thereof
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The invention relates to a compound which is represented by formula I, is used for inhibiting hepatitis C virus, and possesses excellent bioavailability, and a nontoxic pharmaceutically acceptable salt thereof. The compound possesses extremely high inhibition effect on HCV of all genotypes. In the formula I, R is used for representing hydrogen atom, glycyl, L-alanyl, L-leucyl, L-valyl, or L-isoleucyl.
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- Deuterated antiviral active compounds for hepatitis C viruses
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The invention relates to antiviral compounds for hepatitis C viruses (HCVs) and nontoxic pharmacologically-acceptable salts thereof, wherein the compounds are represented by a formula I shown in the description and have good bioavailability, and the compounds have potent inhibiting effects on the all-genotypic HCVs. In the structural formula I, R1, R2, R3 and R4 are independently selected from methyl (-CH3) or deuterated methyl (-CD3); X1, X2, X3, X4 and X5 are separately hydrogen (H) or deuterium (D); and one of the R1, the R2, the R3 and the R4 must be deuterated methyl (-CD3) or one of theX1, the X2, the X3, the X4, and the X5 must be deuterium (D).
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- Preparation of velpatasvir and derivatives thereof
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The invention relates to a preparation method of velpatasvir and derivatives thereof. Concretely, the preparation method provided by the invention comprises the step of preparing the velpatasvir and derivatives thereof (definitions of all the groups are described in the specification) by virtue of an intermediate compound shown in a formula. The preparation method provided by the invention has the advantages that byproducts are fewer, cost is low, and the preparation method is applicable to industrial production of velpatasvir. (The formula is described in the specification.).
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- ANTIVIRAL COMPOUNDS
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The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
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Paragraph 0491
(2013/12/03)
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- CONDENSED IMIDAZOLYLIMIDAZOLES AS ANTIVIRAL COMPOUNDS
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The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
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