478028-16-9

Upstream product

• 116-11-0 2-Methoxypropene 
• 100063-22-7 methyl 3-amino-5-phenylthiophene-2-carboxylate 
• 75-30-9 2-iodo-propane 

Downstream Products

• 942589-57-3 methyl 3-[[(trans-4-methylcyclohexyl)carbonyl](1-methylethyl)amino]-5-phenyl-2-thiophenecarboxylate 
• 712353-33-8 3-[isopropyl-(4-oxo-cyclohexanecarbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid methyl ester 
• 1019338-08-9 methyl 3-[[(4-chloro-2-fluorophenyl)carbonyl]-(1-methylethyl)amino]-5-phenyl-2-thiophenecarboxylate 
• 712353-59-8 3-[isopropyl-(5-methyl-3,6-dihydro-2H-pyran-2-carbonyl)-amino]-5-phenyl-thiophene-2-carboxylic acid methyl ester 
• 712353-44-1 3-[(2-azido-4-methyl-cyclohexanecarbonyl)-isopropyl-amino]-5-phenyl-thiophene-2-carboxylic acid methyl ester 

Relevant academic research and scientific papers

3-CARBONYLAMINOTHIOPHENE-2-CARBOXYLIC ACIDS AS HEPATITIS C VIRUS INHIBITORS

The present invention relates to novel 2-carboxy thiophene compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine, as anti-viral agents. Specifically, the present invention relates to comp

ANTIVIRAL 2-CARBOXY-THIOPHENE COMPOUNDS

Anti-viral agents of compounds of Formula (I) : wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.

Reductive alkylation of aromatic amines with enol ethers

Reductive alkylation of aromatic amines with 2-methoxypropene using 1.0 equivalent of HOAc and NaBH(OAc)3 in 1,2-dichloroethane (DCE) at room temperature furnished N-isopropyl amines in 50-98% yields. This method was successfully extended to trimethylsilyl enol ethers. The mild reaction conditions provide a new alternative procedure for the reductive amination of electron deficient aromatic amines.

Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: Tertiary amides

Further SAR studies on the thiophene-2-carboxylic acids are reported. These studies led to the identification of a series of tertiary amides that show inhibition of both HCV NS5B polymerase in vitro and HCV subgenomic RNA replication in Huh-7 cells. Structural insights about the bioactive conformation of this class of molecules were deduced from a combination of modeling and transferred NOE (trNOE) studies.

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

The present invention provides novel compounds represented by formula (I) or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.