1322758-01-9

Upstream product

• 1322757-53-8 ethyl 3-(4-chlorophenyl)-4-cyano-5-(isopropylsulfonyl)thiophene-2-carboxylate 
• 1322757-80-1 ethyl 5-azido-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylate 
• 1322757-73-2 ethyl 5-amino-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylate 
• 882278-95-7 C₁₇H₁₆ClNO₂S₂ 

Relevant academic research and scientific papers

SNAr and palladium-catalyzed reactions of deactivated thiophene: Application to the synthesis of protein farnesyltransferase inhibitors

To investigate the influence of the 5-thioether moiety of our previously identified hit thiophene compound upon protein farnesyltransferase inhibition, we synthesized a new library of 3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic derivatives through the application of aromatic nucleophilic substitutions benefiting from a sulfone-based leaving group and by direct palladium-catalyzed reactions on a thioalkylthiophene. This small library of ester derivatives and their corresponding acids was then evaluated for protein farnesyltransferase inhibitory activity; some library members exhibited promising submicromolar activities. Copyright