160133-79-9

Upstream product

• 2365-48-2 Methyl thioglycolate 
• 474543-00-5 (Z)-3-Chloro-2-methyl-3-phenyl-acrylonitrile 
• 1078789-34-0 methyl 3-amino-5-bromo-4-methylthiophene-2-carboxylate 
• 98-80-6 phenylboronic acid 
• 17763-67-6 Phenyl triflate 
• 85006-31-1 3-amino-4-methyl-2-thiophenecarboxylic acid methyl ester 
• 108-86-1 bromobenzene 
• 35811-93-9 3-chloro-2-methylcinnamaldehyde 

Downstream Products

• 474543-10-7 3-methyl-5,8-dioxo-2-phenyl-5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine-7-carboxylic acid methyl ester 
• 474543-16-3 3-methyl-2-phenyl-6,7-dihydro-4H-thieno[3,2-b]azepine-5,8-dione 
• 474543-04-9 3-(3-methoxycarbonylpropionylamino)-4-methyl-5-phenylthiophene-2-carboxylic acid methyl ester 

Relevant academic research and scientific papers

EIF4E INHIBITORS AND USES THEREOF

The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.

Palladium-catalyzed direct arylation using free NH2 substituted thiophene derivatives with inhibition of amination type reaction

The palladium-catalyzed direct arylation at C2 or C5 of free NH2 substituted thiophene derivatives was found to proceed in moderate to high yields using a variety of aryl halides. The choice of potassium acetate as the base was found to be crucial to inhibit the amination reaction and to promote the direct arylation.

Synthesis of new thieno[b]azepinediones from α-methylene ketones

New substituted 6,7-dihydro-4H-thieno[3,2-b]azepine-5,8-diones were synthesized in seven steps, starting from substituted α-methylene ketones, via 3-aminothiophene-2-carboxylic acid alkyl esters.