Multitargeting Heterocycles

Nickel-catalyzed tandem isomerization/anti-Markovnikov hydroarylation of unactivated internal alkenes with heteroarenes

“…3 Notably, these linear alkyl-substituted products, particularly for heteroarenes with a linear alkyl substituent at the C2 position, are recognized as privileged structural motifs widely found in natural products, pharmaceuticals, and materials. 4 To the best of our knowledge, the currently developed anti -Markovnikov hydroarylation procedures mostly occur with α-alkenes. In sharp contrast, a similar linear alkylation employing unactivated internal alkenes, an important and abundant class of alkenes, is still challenging 5 because such a transformation can only be achieved by the combination of anti -Markovnikov hydroarylation with a controlled isomerization process of an unactivated internal alkene.…”

Mechanochemistry Frees Thiourea Dioxide (TDO) from the ‘Veils’ of Solvent, Exposing All Its Reactivity

“…Along with the newly synthesized heterocycle, other subproducts were formed. We think their presence was due to the degradative processes of compound 1, as already documented [95,105,106]. Hence, a short silica pad was made to obtain the desired product in high purity.…”

Benzimidazole and its derivatives as cancer therapeutics: The potential role from traditional to precision medicine

“…Nonetheless, substitution at position N will prohibit the tautomerism process 3 . Benzimidazole is a weak base with a p K value at 5.3 and 12.3 for p K a1 and p K a2 , respectively 4 . Therefore, the benzimidazole ring is highly stable and can withstand extreme conditions such as being heated under pressure up to 270 °C in a concentrated sulphuric acid solution or vigorous treatment with hot hydrochloric acid or with alkalis 4 .…”