1007882-23-6

Usage

Uses

(2S,2''S)-2,2''-([1,1''-Biphenyl]-4,4''-diyldi-1H-imidazole-5,2-diyl)bis-1-pyrrolidinecarboxylic Acid 1,1''-Bis(1,1-dimethylethyl) Ester is an antiviral agent and Daclatasvir (D101500) intermediate. Daclatasvir inhibits the HCV protein NS5A and thus can be used as a drug candidate for the treatment of hepatitis C (HCV).

Upstream product

• 14221-01-3 tetrakis(triphenylphosphine) palladium⁽⁰⁾ 
• 1007882-04-3 (S)-tert-butyl 2-(5-(4-bromophenyl)-1H-imidazol-2-yl)pyrrolidine-1-carboxylate 
• 1007882-12-3 (S)-tert-butyl 2-(5-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-1H-imidazol-2-yl)pyrrolidine-1-carboxylate 
• 24860-53-5 1,1’-(biphenyl-4,4’diyl)bis(2-chloroethanone) 
• 69610-41-9 Boc-L-Pro-H 
• 4072-67-7 4,4'-bis(bromoacetyl)biphenyl 
• 5467-72-1 α-amino-4-bromoacetophenone hydrochloride 
• 15761-39-4 1-(tert-butoxycarbonyl)-L-proline 
• 1009119-82-7 1,2-pyrrolidinedicarboxylic acid, 2,2’-[[1,1’-biphenyl]-4,4’-diylbis(2-oxo-2,1-ethanediyl)] bis[1-(1,1-dimethylethyl)] ester, (2S)- 
• 1007881-98-2 y 

Downstream Products

• 1007882-27-0 2-[(2S)-pyrrolidin-2-yl]-5-[4-(4-{2-[(2S)-pyrrolidin-2-yl]-1H-imidazol-5-yl}phenyl)phenyl]-1H-imidazole 
• 1009119-83-8 methyl N-[(2S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate hydrochloride 
• 1312336-87-0 C₃₆H₄₂Br₂N₆O₄ 
• 1388224-19-8 C₃₆H₄₂Cl₂N₆O₄ 
• 1312338-86-5 C₃₆H₄₂I₂N₆O₄ 
• 1388224-20-1 C₃₆H₄₂F₂N₆O₄ 
• 1373165-16-2 C₃₆H₄₃FN₆O₄ 
• 1007884-60-7 methyl N-[(2S)-3-methyl-1-oxo-1-[(2S)-2-{5-[4-(4-{2-[(2S)-pyrrolidin-2-yl]-1H-imidazol-5-yl}phenyl)phenyl]-1H-imidazol-2-yl}pyrrolidin-1-yl]butan-2-yl]carbamate 
• 1009119-83-8 1H-imidazole,5,5'-[1,1'-biphenyl]-4,4'-bis[2-(2S)-2-pyrrolidine-2yl hydrochloride] 

Relevant academic research and scientific papers

Design and synthesis of imidazole N-H substituted amide prodrugs as inhibitors of hepatitis C virus replication

Abstract Twenty-five novel imidazole N-H substituted Daclatasvir (BMS-790052, DCV) analogues (8a-8y) were designed and synthesized as potential prodrugs. Structure modifications were performed in order to improve potency and pharmacokinetic (PK) properties. All target compounds were evaluated in a hepatitis C virus (HCV) genotype 1b replicon, and the 2-oxoethyl acetate substituted compound 8t showed similar anti-HCV activity (EC50 = 0.08 nM) to that of the lead compound Daclatasvir. Moreover, the utility of prodrug 8t was demonstrated through similar exposure of the parent compound when the prodrugs were dosed in vivo. PK studies showed that prodrug 8t was an ideal candidate for a slower and sustained release form of Daclatasvir.

Design, synthesis and evaluation of novel anti-HCV molecules that deliver intracellularly three highly potent NS5A inhibitors

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.

MICRO-ELECTROLYSIS REACTOR FOR ULTRA FAST, OXIDANT FREE, C-C COUPLING REACTION AND SYNTHESIS OF DACLATASVIR ANALOGS THEREOF

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.

Method for preparing imidazole ring intermediate

The invention provides a method for preparing an imidazole ring intermediate and belongs to the field of pharmaceutical and chemical industries. The method disclosed by the invention comprises the following steps: carrying out a condensation reaction on s

PROCESS FOR PREPARATION OF DACLATASVIR AND SALTS

The present invention relates to crystalline daclatasvir dihydrochloride hydrate and process for its preparation.

Preparation method of daclatasvir and its intermediate

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

Anti-hepatitis C Daclatasvir synthesis method

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,

DACLATASVIR FREE BASE AND PROCESS FOR THE PREPARATION THEREOF

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

Synthetic method of daclatasvir

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

PROCESS FOR THE PREPARATION OF AN INTERMEDIATE OF DACLATASVIR DIHYDROCHLORIDE

The present invention provides an improved process for the preparation of 5,5'- biphenyl-4,4'-diylbis{2-[(2S)-pyrrolidin-2-yl]-1H-imidazole}of Formula II and its use for the preparation of daclatasvir dihydrochloride.