Pd-Catalysed [3 + 2]-cycloaddition towards the generation of bioactive bis-heterocycles/identification of COX-2
Elagandhula Sathish1, Arshad J Ansari1,2, Gaurav Joshi3
1School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, NH-8, Ajmer-305801, Rajasthan, India. dms@curaj.ac.in.
Abstract:
In the current research, we envisaged the synthesis of bis-heterocycles containing the dihydroisoxazole ring by [3 + 2] cycloaddition of VECs (vinyl ethylene carbonates) and nitrile oxides, assisted by a Pd catalyst. Herein we explored hydroximoyl chlorides as versatile precursors for the in situ generation of nitrile oxides that were exploited to achieve the cycloaddition reaction on a vinyl group of VECs to generate bis-heterocycles. In silico-based studies of bis-heterocycles on the cyclooxygenase (COX) enzyme displayed selective COX-2 inhibition.
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