A highly efficient and an unprecedented hexafluoro-2-propanol,
promoting low-temperature aromatic nucleophilic substitutions of chloroheteroarenes,
has been performed using thiols and (secondary) amines under base-free
and metal-free conditions. The developed protocol also provides excellent
regio-control for the selective functionalization of dichloroheteroarenes,
while the utility of the protocol was demonstrated by the modification
of a commercially available drug ceritinib.
A highly efficient catalytic protocol for the CÀ H (hetero)arylation of 1,3,4-oxadiazoles using low catalyst loading of Pd/PTABS system with bromo(hetero)arenes has been disclosed. The developed reaction conditions enable the synthesis of a library of differently (hetero)arylated oxadiazoles along with a commercially available fluorescent organic scintillation material, butyl-PBD as well as antitubercular agent PHOXPY. The combination of CÀ H arylation of oxadiazoles with Sonogashira reaction (steroidal substructures bearing alkynes), Heck alkenylation or Suzuki-Miyaura coupling in a one-pot tandem procedure was also made possible with an intent for new drug discovery possibilities.
A highly efficient catalytic protocol for the C–H (hetero)arylation of 1,3,4‐oxadiazoles using a low catalyst loading of a Pd/PTABS system with bromo(hetero)arenes has been disclosed. The reaction conditions developed enable the synthesis of a library of differently (hetero)arylated oxadiazoles along with a commercially available fluorescent organic scintillation material, butyl‐PBD as well as anti‐tubercular agent PHOXPY. A tandem one‐pot sequential C–H arylation/Sonogashira reaction (or with Heck alkenylation or Suzuki–Miyaura coupling) was also made possible. More information can be found in the Full Paper by Anant R. Kapdi et al. on page 289 in Issue 2, 2019 (DOI: 10.1002/ajoc.201800713).
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