Guo, Zhengwei’s team published research in Science China: Chemistry in 62 | CAS: 69626-75-1

Science China: Chemistry published new progress about 69626-75-1. 69626-75-1 belongs to benzofurans, auxiliary class Iodide,Benzofuran, name is 2-Iodobenzofuran, and the molecular formula is C8H5IO, Formula: C8H5IO.

Guo, Zhengwei published the artcileSynthesis of reversible PAD4 inhibitors via copper-catalyzed C-H arylation of benzimidazole, Formula: C8H5IO, the publication is Science China: Chemistry (2019), 62(5), 592-596, database is CAplus.

A Cu-catalyzed C-H arylation reaction of N-heteroarene I [R = H; R1 = H3CO] has been applied to the synthesis of complex non-covalent PAD4 inhibitors I [R = 1-benzyl-1H-indol-2-yl, naphthalen-2-yl, pyrazin-2-yl, etc.; R1 = (3S,4R)-3-amino-4-hydroxypiperidin-1-yl] bearing a bi-heteroaryl pharmacophore. This strategy access various analogs of C2-aryl substituted benzimidazoles I [R1 = OH, H3CO] from a common benzimidazole core I [R = H; R1 = H3CO] and easily accessible aryl iodides RI. Preliminary SAR studies revealed that the indole motif of GSK-484 is critical to its activity. Replacing the N-cyclopropylmethyl group to N-benzyl group on the indole ring of GSK-484 resulted in more than 5-fold increase in cell killing efficacy against 4T1 cell line.

Science China: Chemistry published new progress about 69626-75-1. 69626-75-1 belongs to benzofurans, auxiliary class Iodide,Benzofuran, name is 2-Iodobenzofuran, and the molecular formula is C8H5IO, Formula: C8H5IO.

Referemce:
https://en.wikipedia.org/wiki/Benzofuran,
Benzofuran | C8H6O – PubChem