01311nas a2200241 4500008004100000022001400041245008500055210006900140260000900209300001400218490000700232520053600239653001900775653003500794653001600829653001200845653001700857653001300874100002600887700002400913700002400937856010800961 2023 eng d a0039-788100aRh-catalyzed C-H functionalization of the (Pyrazol-5-yl)pyridine core of GBT-4400 aRhcatalyzed CH functionalization of the Pyrazol5ylpyridine core  cNOV  a3600-36090 v553 a

The Rh-catalyzed cross dehydrogenative coupling (CDC)/alkylation of the pyrazolylpyridine unit of GBT-440 proceeded smoothly under ambient conditions and selectively on the pyrazole unit while directed by the pyridine. The scope of these reactions was established by employing simple as well as conjugated olefins for CDC and various diazo esters and the TIPS-EBX reagent for alkylation. At the outset, a focused small molecule library around the bis-heterocyclic core of GBT440 was developed via C-H functionalization.

10aC-H activation10across dehydrogenative coupling10adiazo ester10aGBT-44010aRh catalysis10aTIPS-EBX1 aKalshetti, Rupali, G.1 aHalnor, Swapnil, V.1 aRamana, Chepuri, V. uhttps://library.ncl.res.in/content/rh-catalyzed-c-h-functionalization-pyrazol-5-ylpyridine-core-gbt-440