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.
Allyltrimethylsilane inspired allylation of acetals, ketals, aldehydes, and ketones comprises one of the most viable, significant and graceful methods for the formation of carbon–carbon bonds leading to stereochemical transformation.
A novel I-promoted direct conversion of arylacetic acids into aryl carboxylic acids under metal-free conditions has been described. This remarkable transformation involves decarboxylation followed by an oxidation reaction enabled just by using DMSO as the solvent as well as an oxidant. Notably, aryl carboxylic acids are isolated by simple filtration technique and obtained in good to excellent yields. This protocol is free from chromatographic purification, which makes it applicable for large-scale synthesis.
Review covering the synthesis of 5- and 6-membered as well as condensed heteroarenes, focussing on the combinations in cooperative catalytic systems in strategies used to achieve selectivity and also highlights the mode of action for the cooperative catalysis leading to the synthesis of commercially and biologically relevant heteroarenes.
A new metal-free tandem protocol for the synthesis of α-ketoimides via sp3, sp2, and sp C–H functionalization followed by oxidative cross coupling with benzamidines hydrochloride using catalytic iodine with TBHP in DMSO has been developed.
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