944644-86-4

Upstream product

• 18791-75-8 4-Bromothiophen-2-aldehyde 
• 13139-86-1 4-methoxyphenyl magnesium bromide 
• 14774-77-7 p-methoxyphenyllithium 

Downstream Products

• 1377891-48-9 (1S)-1,5-anhydro-2,3,4,6-tetra-O-benzyl-1-[5-(4-methoxybenzyl)-3-thienyl]-D-glucitol 
• 1377891-35-4 (1S)-1,5-anhydro-1-[5-(4-methoxybenzyl)-3-thienyl]-D-glucitol 
• 1377891-45-6 4-bromo-2-(4-methoxybenzyl)thiophene 
• 1026433-93-1 5-[(4-Methoxy-phenyl)-trimethylsilanyloxy-methyl]-thiophene-3-sulfonyl chloride 
• 1026583-33-4 5-[(4-Methoxy-phenyl)-trimethylsilanyloxy-methyl]-thiophene-3-sulfonic acid amide 
• 155954-68-0 5-<1-hydroxy-1-(4-methoxyphenyl)methyl>-3-thiophenesulfonamide 

Relevant academic research and scientific papers

Discovery of Ipragliflozin (ASP1941): A novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus

A series of C-glucosides with various heteroaromatics has been synthesized and its inhibitory activity toward SGLTs was evaluated. Upon screening several compounds, the benzothiophene derivative (14a) was found to have potent inhibitory activity against SGLT2 and good selectivity versus SGLT1. Through further optimization of 14a, a novel benzothiophene derivative (14h; ipragliflozin, ASP1941) was discovered as a highly potent and selective SGLT2 inhibitor that reduced blood glucose levels in a dose-dependent manner in diabetic models KK-Ay mice and STZ rats.

5-Substituted 3-thiophenesulfonamides as carbonic anhydrase inhibitors

A series of 5-substituted 3-thiophenesulfonamides was prepared from 4-bromo-2-thiophene carboxaldehyde. Several of these compounds inhibited carbonic anhydrase II in vitro at concentrations of less than 10 nM. In the ex vivo assay, these compounds have inhibitory values in the 25-81% range. Additionally, none of these compounds exhibit sensitization potential as determined by in vitro measurement of cysteine reactivity.