An efficient metal-free one-pot protocol has been developed for the construction of 1,3,4-oxadiazole derivatives via iodine-mediated oxidative amination of benzylic C–H bonds of azaarenes.

No abstract

No abstract

A novel strategy towards the synthesis of 1,4-disubstituted 1,2,3-triazoles via C–N and N–N bond formation has been demonstrated under transition metal-free and azide-free conditions.

No abstract

A facile iodine-mediated unprecedented C-C cleavage by employing CuI has been established towards the synthesis of quinazolin-4(3H)-ones and benzo [4,5]imidazo[1,2-c]quinazolines. This protocol involves peroxide free synthetic approach for the stable C-C bond cleavage followed by oxidative annulation to develop a library of fused N-heterocyclic molecules.

Background: Discovery of small molecules that inhibit tubulin polymerization is an attractive strategy for the development of new and improved anti-proliferative agents. Objective: A series of novel 2-sulfonyl-1,1-diarylethenes were designed towards this end keeping in view of the favorable chemical and pharmacological virtues of unsaturated sulfones. Methods: Rapid, convenient and efficient two-step assembly of the designed molecules was achieved by the vicinal iodosulfonylation-Suzuki coupling sequence. Results: As hypothesized, these compounds showed good anti-proliferative activity against different tissue-specific cancer cell lines: MCF-7, DU-145, A-549, HepG2, and HeLa. The most active compound, p-nitrophenyl ring-bearing analog, exhibited an IC50 value of 0.90µM against A-549 cells. Flow cytometry studies on this derivative revealed that it arrests the cell cycle of A-549 cells at the G2/M phase. This compound exhibited molecular binding to tubulin as well as tubulin polymerization inhibition comparable to that of colchicine. Conclusion: A new class of potent, tubulin binding anticancer agents based on 1,1,-diarylvinyl sulfone scaffold has been designed and synthesized.

An iodine promoted tandem oxidative condensation of benzylamines and 2-methylquinazolin-4-(3H)-ones was developed to yield imidazo[1,5-a]quinazolin-5(4H)-ones via dual C(sp)-H amination under metal free conditions in a greener way using molecular oxygen as a terminal oxidant. This tandem transformation provides an efficient approach to construct various functionalized imidazo[1,5-a]quinazolin-5(4H)-ones in a straightforward manner via a sequential amination-oxidation-annulation-aromatisation.