- A antiviral drug intermediate resolution method
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The invention relates to a method for splitting an antiviral drug intermediate, and particularly relates to a method for splitting (2S)-1-(t-butyloxycarboryl)-4-(methoxymethyl)-pyrrolidine-2-carboxylic acid. According to the method, (2S,4S)-1-(t-butyloxyc
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Paragraph 0041; 0042
(2019/02/26)
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- Preparation method of hepatitis c virus resisting medicine key intermediate
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The invention discloses a preparation method of a hepatitis c virus resisting medicine key intermediate (4S)-N-Boc-4-methoxymethyl-L-proline. The preparation method comprises the following steps: under the action of an acid binding agent, enabling 4S-hydr
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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 method of anti-virus drug intermediate
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The invention discloses a preparation method of an anti-virus drug intermediate. A structure of the intermediate corresponds to a formula V: the formula V is shown in the description. The method comprises the following steps: carrying out reaction in four steps: condensation, reduction, dissociation and splitting on a compound (2S)-N-Boc-4-methoxymethylene pyrrolidine-2-carboxylic acid used as a raw material to finally obtain a (4S)-N-Boc-methoxymethyl-L-proline shown in the formula V. The method disclosed by the invention has cheap and easily-available raw materials, reaction conditions are mild, the selective problem is avoided, the yield is higher, and the method is more suitable for industrial production. The preparation method provided by the invention is high in asymmetric hydrogenation selectivity, simple in splitting conditions, mild in reaction conditions, higher in yield, and suitable for industrial amplified production.
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- (4S)-N-Boc-4-methoxymethyl-L-proline synthesis method
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The invention discloses a (4S)-N-Boc-4-methoxymethyl-L-proline synthesis method. The method comprises that 1, L-hydroxyproline as an initial raw material is subjected to Boc protection so that N-Boc-L-hydroxyproline is produced, 2, the N-Boc-L-hydroxyproline is dissolved in a solvent, the solution and 2, 2, 6, 6-tetramethyl-1-piperidinyloxy (TEMPO) undergo an oxidation reaction to produce (2S)-N-Boc-4-oxopyrrolidine-2-carboxylic acid, 3, the (2S)-N-Boc-4-oxopyrrolidine-2-carboxylic acid and (methoxymethyl)triphenylphosphonium chloride are dissolved in a solvent and undergo a wittig reaction to produce (2S)-N-Boc-4-methoxymethylenepyrrolidine-2-carboxylic acid, and 4, the (2S)-N-Boc-4-methoxymethylenepyrrolidine-2-carboxylic acid and tert-butylamine are dissolved in water and undergo a hydrogenation reaction to produce (4S)-N-Boc-4-methoxymethyl-L-proline. The method shortens reaction processes, is free of severe-toxicity cyanides, improves safety, reduces environmental protection pressure, improves atom economy, reduces waste discharge and greatly reduces a raw material cost.
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Paragraph 0066; 0067
(2016/10/31)
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- Preparation method for pyrrolidine-2-carboxylic acid derivatives
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The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R1 or R2, R1 is C1-C6 an alkyl, benzyl, p-methoxybenzyl, or p-nitrobenzyl group, and R2 is hydrogen; R3 is a protecting group of the carboxyl group; and P1 is a protecting group on nitrogen.
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- PROCESSES FOR PREPARING ANTIVIRAL COMPOUNDS
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The present disclosure provides processes for the preparation of a compound of formula: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates.
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Paragraph 0405
(2015/12/30)
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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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- 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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- 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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- 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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- HEPATITIS C VIRUS INHIBITORS
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The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
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Paragraph 0475
(2013/05/21)
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