A Green Synthesis of 1,5-Benzodiazepines using Reusable-Heterogeneous Silica Sulfuric
Acid Catalyst under Solvent-Free Conditions and their Antileukemic Activity
1,5-Benzodiazepine derivatives are readily assembled from o-phenylene diamine and ketones containg α-hydrogen atoms by means of simple cyclocondensation via sp3 C-H activation promoted by an efficient heterogeneous silica sulfuric acid catalyst. Eco-friendliness, good yields, easy workup, reusable catalyst, short reaction times, high atom economy and solvent-free conditions are the noteworthy features of this protocol. These benzodiazepines are chosen for the evaluation of antiproliferative activity against different leukemia cell lines. Among the investigated compounds, 3g is the best antiproliferative agent against all the cell lines tested. Also, current preliminary analysis showed that compound 3g phosphorylates ERK1/2 and induces G1 arrest in K562 cells