- MICRO-ELECTROLYSIS REACTOR FOR ULTRA FAST, OXIDANT FREE, C-C COUPLING REACTION AND SYNTHESIS OF DACLATASVIR ANALOGS THEREOF
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The present invention relates to a continuous micro-electro-flow reactor system for ultra-fast, oxidant free, C—C coupling reaction for making symmetrical biaryls and analogs thereof. This invention further relates to the said process for preparation of antiviral drug, daclatasvir of general formula I.
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- PROCESS FOR PREPARATION OF DACLATASVIR AND SALTS
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The present invention relates to crystalline daclatasvir dihydrochloride hydrate and process for its preparation.
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- Synthetic method of daclatasvir
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The invention discloses a synthetic method of daclatasvir. The method adopts bis(2-bromoacetyl) biphenyl and t-butyloxycarboryl-L-proline as initial raw materials, the initial raw materials are separately synthesized into a midbody N-4, N-3, N-2 and N-1 i
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Paragraph 0020
(2018/01/11)
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- Preparation method of daclatasvir and its intermediate
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The invention discloses a preparation method of daclatasvir and its intermediate. The invention provides a preparation method of a daclatasvir intermediate I. The method includes the step of: in an organic solvent or under a solvent-free condition, subjec
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Paragraph 0043; 0061; 0073-0079; 0085; 0086; 0089-0091
(2017/08/28)
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- Anti-hepatitis C Daclatasvir synthesis method
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The invention discloses an anti-hepatitis C Daclatasvir synthesis method. The anti-hepatitis C Daclatasvir synthesis method comprises the following steps that 1, 4,4'-di(2-chloracetyl) biphenyl and Boc-L-proline perform condensation to generate ester; 2,
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Paragraph 0093-0094
(2017/04/03)
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- DACLATASVIR FREE BASE AND PROCESS FOR THE PREPARATION THEREOF
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The present invention relates to daclatasvir free base, processes for its preparation, a process for its conversion into pharmaceutically acceptable salts of daclatasvir. The present invention also relates to a process for the preparation and purification
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Page/Page column 23
(2017/03/08)
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- Novel method for synthesizing dimethyl dicarbamate dihydrochloride compound
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The invention relates to a novel method for synthesizing N,N'[[1,1'-biphenyl]4, 4'-diyl bis[1H-imidazole-5,2-diyl-(2S)-2,1-pyrrolidinediyl[(1S)-1-(1-ethylmethyl)-2-oxo-2,1-ethanediyl]]] dimethyl dicarbamate dihydrochloride. According to the novel method d
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Paragraph 0031; 0032
(2016/10/10)
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- PROCESS FOR THE PREPARATION OF DACLATASVIR
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The present disclosure provides a novel process for the preparation of daclatasvir or pharmaceutically acceptable salts thereof using novel intermediates. Formula (I)
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Page/Page column 25-26
(2016/11/21)
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- Design, synthesis and evaluation of novel anti-HCV molecules that deliver intracellularly three highly potent NS5A inhibitors
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The design and synthesis of new non-symmetrical NS5A inhibitors with sulfur containing amino acids is reported along with their ability to block HCV replication in an HCV 1b replicon system. These compounds display EC50 values in the picomolar range with a large therapeutic index (>106). Moreover, cellular pharmacology studies show that our preferred compounds intracellularly deliver three potent NS5A inhibitors.
- Boucle, Sebastien,Tao, Sijia,Amblard, Franck,Stanton, Richard A.,Nettles, James H.,Li, Chengwei,McBrayer, Tamara R.,Whitaker, Tony,Coats, Steven J.,Schinazi, Raymond F.
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p. 3711 - 3715
(2015/08/11)
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- CRYSTALLINE FORM OF METHYL ((1S)-1-(((2S)-2-(5-(4'-(2-((2S)-1-((2S)-2-((METHOXYCARBONYL)AMINO)-3-METHYLBUTANOYL)-2-PYRROLIDINYL)-1H-IMIDAZOL-5-YL)-4-BIPHENYLYL)-1H-IMIDAZOL-2-YL)-1-PYRROLIDINYL)CARBONYL)-2-METHYLPROPYL)CARBAMATE DIHYDROCHLORIDE SALT
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The present disclosure generally relates to a crystalline form of methyl ((1S)-1-(((2S)-2-(5-(4'-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1 H-imidazol-5-yl)-4-biphenylyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt. The present disclosure also generally relates to a pharmaceutical composition comprising a crystalline form, as well as methods of using a crystalline form in the treatment of Hepatitis C and methods for obtaining such crystalline form.
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Paragraph 0140-0142; 0144
(2016/12/16)
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- HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 149
(2010/12/26)
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- Process for Synthesizing Compounds Useful for Treating Hepatitis C
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The present disclosure generally relates to a process for synthesizing methyl ((1S)-1-(((2S)-2-(5-(4′-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3- methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-5-yl)-4-biphenylyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt. The present disclosure also generally relates to intermediates useful in this process.
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Page/Page column 9
(2009/03/07)
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- Hepatitis C Virus Inhibitors
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The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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